Shah, Shafiq Ali et al. published their research in Tropical Journal of Pharmaceutical Research in 2018 | CAS: 1222780-33-7

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Vasodilator effect of 1-trifluoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea is predominantly mediated through activation of voltage-dependent K+ channels was written by Shah, Shafiq Ali;Mehmood, Malik Hassan;Khan, Munasib;Bukhari, Ishfaq Ali;Gilani, Anwarul Hassan. And the article was included in Tropical Journal of Pharmaceutical Research in 2018.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

To determine the mechanism of vasorelaxant effect of 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea in cardiovascular diseases, including hypertension. Isolated rat thoracic aortic tissue preparations were mounted in an organ bath set up integrated with isometric transducer and a Power Lab assembly. TPPU was tested for vasorelaxant effect against low K+ (25 mM) and high K+ (80 mM)-induced contractions and its mechanism was determined in the presence of different antagonists (glibenclamide, 4- aminopyridine and tetra-Et ammonium). In rat aortic preparations, TPPU showed a concentration-dependent (0.3 – 100μM) and significant (p < 0.001) inhibition of low K+ induced contractions with complete inhibition obtained at 100μM. TPPU produced significant inhibition of high K+ induced contractions with maximum relaxation of 15.36 ± 1.95% and 15.85 ± 3.35% at 30 and 100μM, resp. Glibenclamide (Gb,10μM) pretreatment partially inhibited the vasorelaxant effect of TPPU against low K+ in a concentration range of 1 – 30μM. 4-Aminopyridine (4-AP, 1 mM) and tetra-Et ammonium markedly inhibited the vasorelexant effect of TPPU against low K+ induced contractions with maximum relaxation of 20.09 ± 2.40 and 21.67 ± 0.88%, resp., at 100μM. TPPU possesses marked vasorelaxant properties which provides sound pharmacol. evidence for its use as a potential drug candidate in the management of hypertension. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Maillard, Michel C. et al. published their research in Bioorganic & Medicinal Chemistry in 2011 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Reference of 86069-86-5

Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: Structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors was written by Maillard, Michel C.;Brookfield, Frederick A.;Courtney, Stephen M.;Eustache, Florence M.;Gemkow, Mark J.;Handel, Rebecca K.;Johnson, Laura C.;Johnson, Peter D.;Kerry, Mark A.;Krieger, Florian;Meniconi, Mirco;Munoz-Sanjuan, Ignacio;Palfrey, Jordan J.;Park, Hyunsun;Schaertl, Sabine;Taylor, Malcolm G.;Weddell, Derek;Dominguez, Celia. And the article was included in Bioorganic & Medicinal Chemistry in 2011.Reference of 86069-86-5 The following contents are mentioned in the article:

Several caspases have been implicated in the pathogenesis of Huntington’s disease (HD); however, existing caspase inhibitors lack the selectivity required to investigate the specific involvement of individual caspases in the neuronal cell death associated with HD. In order to explore the potential role played by caspase-2, the potent but non-selective canonical Ac-VDVAD-CHO caspase-2 inhibitor 1 was rationally modified at the P2 residue in an attempt to decrease its activity against caspase-3. With the aid of structural information on the caspase-2, and -3 active sites and mol. modeling, a 3-(S)-substituted-L-proline along with four addnl. scaffold variants were selected as P2 elements for their predicted ability to clash sterically with a residue of the caspase-3 S2 pocket. These elements were then incorporated by solid-phase synthesis into pentapeptide aldehydes 33av. Proline-based compound 33h bearing a bulky 3-(S)-substituent displayed advantageous characteristics in biochem. and cellular assays with 20- to 60-fold increased selectivity for caspase-2 and ∼200-fold decreased caspase-3 potency compared to the reference inhibitor 1. Further optimization of this prototype compound may lead to the discovery of valuable pharmacol. tools for the study of caspase-2 mediated cell death, particularly as it relates to HD. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Reference of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.Reference of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Maillard, Michel C. et al. published their research in Bioorganic & Medicinal Chemistry in 2011 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: Structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors was written by Maillard, Michel C.;Brookfield, Frederick A.;Courtney, Stephen M.;Eustache, Florence M.;Gemkow, Mark J.;Handel, Rebecca K.;Johnson, Laura C.;Johnson, Peter D.;Kerry, Mark A.;Krieger, Florian;Meniconi, Mirco;Munoz-Sanjuan, Ignacio;Palfrey, Jordan J.;Park, Hyunsun;Schaertl, Sabine;Taylor, Malcolm G.;Weddell, Derek;Dominguez, Celia. And the article was included in Bioorganic & Medicinal Chemistry in 2011.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Several caspases have been implicated in the pathogenesis of Huntington’s disease (HD); however, existing caspase inhibitors lack the selectivity required to investigate the specific involvement of individual caspases in the neuronal cell death associated with HD. In order to explore the potential role played by caspase-2, the potent but non-selective canonical Ac-VDVAD-CHO caspase-2 inhibitor 1 was rationally modified at the P2 residue in an attempt to decrease its activity against caspase-3. With the aid of structural information on the caspase-2, and -3 active sites and mol. modeling, a 3-(S)-substituted-L-proline along with four addnl. scaffold variants were selected as P2 elements for their predicted ability to clash sterically with a residue of the caspase-3 S2 pocket. These elements were then incorporated by solid-phase synthesis into pentapeptide aldehydes 33av. Proline-based compound 33h bearing a bulky 3-(S)-substituent displayed advantageous characteristics in biochem. and cellular assays with 20- to 60-fold increased selectivity for caspase-2 and ∼200-fold decreased caspase-3 potency compared to the reference inhibitor 1. Further optimization of this prototype compound may lead to the discovery of valuable pharmacol. tools for the study of caspase-2 mediated cell death, particularly as it relates to HD. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Maier, Norbert M. et al. published their research in Acta Chimica Slovenica in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 86069-86-5

Chromatographic enantiomer separation using 9-amino-9-(deoxy)-epiquinine-derived chiral selectors: control of chiral recognition via introduction of additional stereogenic centers was written by Maier, Norbert M.;Greco, Elisa;Petrovaj, Jan;Lindner, Wolfgang. And the article was included in Acta Chimica Slovenica in 2012.Application of 86069-86-5 The following contents are mentioned in the article:

Three new cinchona-type chiral selectors were prepared by attaching N-pivaloyl-glycine, N-pivaloyl-(S)-valine and N-pivaloyl-(R)-valine segments to the C9-amino function of 9-amino-9-(deoxy)-epiquinine (eAQN), and immobilized to silica to provide the corresponding chiral stationary phases (CSPs). Evaluation of the chromatog. enantioseparation characteristics of these CSPs with a broad assortment of N-carbamoyl protected amino acids under polar organic mobile phase conditions revealed modest chiral recognition capabilities for N-Fmoc-, N-Cbz- and N-Boc-derivatives The enantioselective analyte binding to these CSPs is strictly controlled by the absolute stereochem. of the amino acid functionalities attached to the C9-amino group of the eAQN framework. Specifically, the CSP derived from (S)-valine-based selector exhibits preferential binding of N-carbamoyl-(S)-amino acids, while the CSPs featuring (R)-valine- and the glycine-derived selectors show opposite enantioselective binding preference. The observed impact of analyte structure on enantioselectivity and the specific preferences in enantioselective binding point to chiral recognition mechanisms capitalizing on intermol. ion pairing, hydrogen bonding and subtle steric interactions, with the latter making the crucial contributions to stereodiscrimination. The finding that the chiral recognition characteristics of epiquinine can be readily controlled via incorporation of addnl. stereogenic centers remote from the cinchona scaffold might be useful information for the design of new enantioselective receptors and organocatalysts. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Application of 86069-86-5).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Maier, Norbert M. et al. published their research in Acta Chimica Slovenica in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Category: piperidines

Chromatographic enantiomer separation using 9-amino-9-(deoxy)-epiquinine-derived chiral selectors: control of chiral recognition via introduction of additional stereogenic centers was written by Maier, Norbert M.;Greco, Elisa;Petrovaj, Jan;Lindner, Wolfgang. And the article was included in Acta Chimica Slovenica in 2012.Category: piperidines The following contents are mentioned in the article:

Three new cinchona-type chiral selectors were prepared by attaching N-pivaloyl-glycine, N-pivaloyl-(S)-valine and N-pivaloyl-(R)-valine segments to the C9-amino function of 9-amino-9-(deoxy)-epiquinine (eAQN), and immobilized to silica to provide the corresponding chiral stationary phases (CSPs). Evaluation of the chromatog. enantioseparation characteristics of these CSPs with a broad assortment of N-carbamoyl protected amino acids under polar organic mobile phase conditions revealed modest chiral recognition capabilities for N-Fmoc-, N-Cbz- and N-Boc-derivatives The enantioselective analyte binding to these CSPs is strictly controlled by the absolute stereochem. of the amino acid functionalities attached to the C9-amino group of the eAQN framework. Specifically, the CSP derived from (S)-valine-based selector exhibits preferential binding of N-carbamoyl-(S)-amino acids, while the CSPs featuring (R)-valine- and the glycine-derived selectors show opposite enantioselective binding preference. The observed impact of analyte structure on enantioselectivity and the specific preferences in enantioselective binding point to chiral recognition mechanisms capitalizing on intermol. ion pairing, hydrogen bonding and subtle steric interactions, with the latter making the crucial contributions to stereodiscrimination. The finding that the chiral recognition characteristics of epiquinine can be readily controlled via incorporation of addnl. stereogenic centers remote from the cinchona scaffold might be useful information for the design of new enantioselective receptors and organocatalysts. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Category: piperidines).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Lee, Jiyoun et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Synthetic Route of C21H21NO4

Synthesis and evaluation of aza-peptidyl inhibitors of the lysosomal asparaginyl endopeptidase, legumain was written by Lee, Jiyoun;Bogyo, Matthew. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

Legumain or asparaginyl endopeptidase (AEP) is a lysosomal cysteine protease with a high level of specificity for cleavage of protein substrates after an asparagine residue. It is also capable of cleaving after aspartic acids sites when in the acidic environment of the lysosome. Legumain expression and activity is linked to a number of pathol. conditions including cancer, atherosclerosis and inflammation, yet its biol. role in these pathologies is not well-understood. Highly potent and selective inhibitors of legumain would not only be valuable for studying the functional roles of legumain in these conditions, but may have therapeutic potential as well. The authors describe here the design, synthesis and in vitro evaluation of selective legumain inhibitors based on the aza-asparaginyl scaffold. The authors synthesized a library of aza-peptidyl inhibitors with various non-natural amino acids and different electrophilic warheads, and characterized the kinetic properties of inactivation of legumain. The authors also synthesized fluorescently labeled inhibitors to investigate cell permeability and selectivity of the compounds The inhibitors have second order rate constants of up to 5 × 104 M-1 s-1 and IC50 values as low as 4 nM against recombinant mouse legumain. In addition, the inhibitors are highly selective toward legumain and have little or no cross-reactivity with cathepsins. Overall, the authors have identified several valuable new inhibitors of legumain that can be used to study legumain function in multiple disease models. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Synthetic Route of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Lee, Jiyoun et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Synthesis and evaluation of aza-peptidyl inhibitors of the lysosomal asparaginyl endopeptidase, legumain was written by Lee, Jiyoun;Bogyo, Matthew. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid The following contents are mentioned in the article:

Legumain or asparaginyl endopeptidase (AEP) is a lysosomal cysteine protease with a high level of specificity for cleavage of protein substrates after an asparagine residue. It is also capable of cleaving after aspartic acids sites when in the acidic environment of the lysosome. Legumain expression and activity is linked to a number of pathol. conditions including cancer, atherosclerosis and inflammation, yet its biol. role in these pathologies is not well-understood. Highly potent and selective inhibitors of legumain would not only be valuable for studying the functional roles of legumain in these conditions, but may have therapeutic potential as well. The authors describe here the design, synthesis and in vitro evaluation of selective legumain inhibitors based on the aza-asparaginyl scaffold. The authors synthesized a library of aza-peptidyl inhibitors with various non-natural amino acids and different electrophilic warheads, and characterized the kinetic properties of inactivation of legumain. The authors also synthesized fluorescently labeled inhibitors to investigate cell permeability and selectivity of the compounds The inhibitors have second order rate constants of up to 5 × 104 M-1 s-1 and IC50 values as low as 4 nM against recombinant mouse legumain. In addition, the inhibitors are highly selective toward legumain and have little or no cross-reactivity with cathepsins. Overall, the authors have identified several valuable new inhibitors of legumain that can be used to study legumain function in multiple disease models. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Safety of (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Zhou, Chi et al. published their research in Alcoholism: Clinical & Experimental Research in 2018 | CAS: 1222780-33-7

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Pharmacological Inhibition of Soluble Epoxide Hydrolase Ameliorates Chronic Ethanol-Induced Cardiac Fibrosis by Restoring Autophagic Flux was written by Zhou, Chi;Huang, Jin;Li, Qing;Zhan, Chenao;He, Ying;Liu, Jinyan;Wen, Zheng;Wang, Dao Wen. And the article was included in Alcoholism: Clinical & Experimental Research in 2018.Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

Background : Chronic drinking leads to myocardial contractile dysfunction and dilated cardiomyopathy, and cardiac fibrosis is a consequence of these alc. injuries. Soluble epoxide hydrolase (sEH) hydrolyzes epoxyeicosatrienoic acids (EETs) to less bioactive diols, and EETs have cardioprotective properties. However, the effects of sEH inhibition in ethanol (EtOH)-induced cardiac fibrosis are unknown. Methods : This study was designed to investigate the role and underlying mechanisms of sEH inhibition in chronic EtOH feeding-induced cardiac fibrosis. C57BL/6J mice were fed a 4% Lieber-DeCarli EtOH diet for 8 wk, and the sEH inhibitor 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) was administered throughout the exptl. period. Results : The results showed that chronic EtOH intake led to cardiac dilatation, collagen deposition, and autophagosome accumulation, while TPPU administration ameliorated these effects. In vitro, treating primary cardiac fibroblasts (CFs) with EtOH resulted in CF activation, including alpha smooth muscle actin overexpression, collagen synthesis, and cell migration. Moreover, EtOH disturbed CF autophagic flux, as evidenced by the increased LC3 II/I ratio and SQSTM1 expression, and by the enhanced autophagosome accumulation. TPPU treatment prevented the activation of CF induced by EtOH and restored the impaired autophagic flux by suppressing mTOR activation. Conclusions : Taken together, these findings suggest that sEH pharmacol. inhibition may be a unique therapeutic strategy for treating EtOH-induced cardiac fibrosis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Safety of 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Wang, Xiaojing et al. published their research in Scandinavian Journal of Immunology in 2019 | CAS: 1222780-33-7

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.SDS of cas: 1222780-33-7

Epoxyeicosatrienoic acids alleviate methionine-choline-deficient diet-induced non-alcoholic steatohepatitis in mice was written by Wang, Xiaojing;Li, Lan;Wang, Hongwu;Xiao, Fang;Ning, Qin. And the article was included in Scandinavian Journal of Immunology in 2019.SDS of cas: 1222780-33-7 The following contents are mentioned in the article:

The epoxyeicosatrienoic acids (EETs) are products of cytochrome P 450 epoxygenases and have recently been found to have an anti-inflammatory activity. However, the role of EETs in non-alc. steatohepatitis has not been fully understood. In this study, we investigated the protective role of EETs in methionine-choline-deficient (MCD) diet-induced non-alc. steatohepatitis (NASH) in mice and the potential mechanisms. We used 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl)urea(TPPU), a soluble epoxide hydrolase inhibitor, to increase the endogenous EET level in mice. Upon TPPU treatment, the liver steatosis and inflammatory damage were significantly ameliorated in mice with steatohepatitis, paralleled by the downregulation of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) as well as chemokines (CXCL1, MCP-1). Compared with untreated NASH mice, mRNA levels of sterol regulatory element binding protein 1c (SREBP1c) and inflammation relevant adhesion mols. (ICAM-1, VCAM-1) were downregulated, whereas mRNA level of peroxisome proliferator-activated receptor α(PPAR-α) was elevated in TPPU-treated mice. In vitro, 11,12-EET treatment remarkably attenuated free fatty acid (FFA)-induced inflammation in HepG2 and THP-1 cells. Further, 11,12-EET inhibited the activation of NF-kappaB signalling pathway in macrophages from mice with steatohepatitis. Collectively, these results suggest that EETs play a protective role and alleviate the MCD diet-induced steatohepatitis in mice mainly by downregulating activation of NF-κB pathway in macrophages. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7SDS of cas: 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N–H bond in an axial position, and the other in an equatorial position.SDS of cas: 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Liu, Tao et al. published their research in ACS Combinatorial Science in 2011 | CAS: 86069-86-5

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Electric Literature of C21H21NO4

High-Throughput Screening of One-Bead-One-Compound Libraries: Identification of Cyclic Peptidyl Inhibitors against Calcineurin/NFAT Interaction was written by Liu, Tao;Qian, Ziqing;Xiao, Qing;Pei, Dehua. And the article was included in ACS Combinatorial Science in 2011.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

One-bead-one-compound (OBOC) libraries provide a powerful tool for drug discovery as well as biomedical research. However, screening a large number of beads/compounds (>1 million) and rank ordering the initial hits (which are covalently attached to a solid support) according to their potencies still pose significant tech. challenges. In this work, we have integrated some of the latest tech. advances from our own as well as other laboratories to develop a general methodol. for rapidly screening large OBOC libraries. The methodol. has been applied to synthesize and screen a cyclic peptide library that features: (1) spatially segregated beads containing cyclic peptides on the surface layer and linear encoding peptides in their interior; (2) rapid on-bead screening of the library (>1 million) by a multistage procedure (magnetic bead sorting, enzyme-linked assay, and fluorescence based screening); (3) selective release of cyclic peptides from single pos. beads for solution-phase determination of their binding affinities; and (4) hit identification by partial Edman degradation/mass spectrometry (PED/MS). Screening of the library against protein phosphatase calcineurin (Cn) identified a series of cyclic peptides that bind to the substrate-docking site for nuclear factor of activated T cells (NFAT) with KD values of ∼1 μM. Further improvement of the affinity and specificity of these compounds may lead to a new class of immunosuppressive agents that are more selective and therefore less toxic than cyclosporine A and FK506. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).

(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine has a role as a reagent, a protic solvent, a base, a catalyst, a plant metabolite, a human metabolite and a non-polar solvent. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem