Tag: 300-400

Parallel imaging of coagulation pathway proteases activated protein C, thrombin, and factor Xa in human plasma was written by Modrzycka, Sylwia;Kolt, Sonia;Polderdijk, Stephanie G. I.;Adams, Ty E.;Potoczek, Stanislaw;Huntington, James A.;Kasperkiewicz, Paulina;Drag, Marcin. And the article was included in Chemical Science in 2022.SDS of cas: 86069-86-5 The following contents are mentioned in the article:

Activated protein C (APC), thrombin, and factor (f) Xa are vitamin K-dependent serine proteases that are key factors in blood coagulation. Moreover, they play important roles in inflammation, apoptosis, fibrosis, angiogenesis, and viral infections. Abnormal activity of these coagulation factors has been related to multiple conditions, such as bleeding and thrombosis, Alzheimer鈥瞫 disease, sepsis, multiple sclerosis, and COVID-19. The individual activities of APC, thrombin, and fXa in coagulation and in various diseases are difficult to establish since these proteases are related and have similar substrate preferences. Therefore, the development of selective chem. tools that enable imaging and discrimination between coagulation factors in biol. samples may provide better insight into their roles in various conditions and potentially aid in the establishment of novel diagnostic tests. In our study, we used a large collection of unnatural amino acids, and this enabled us to extensively explore the binding pockets of the enzymes鈥?active sites. Based on the specificity profiles obtained, we designed highly selective substrates, inhibitors, and fluorescent activity-based probes (ABPs) that were used for fast, direct, and simultaneous detection of APC, thrombin, and fXa in human plasma. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5SDS of 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. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.SDS of cas: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Solid-phase synthesis of 2,3,5-triketopiperadine was written by Makino, Shingo;Nakanishi, Eiji;Tsuji, Takashi. And the article was included in Synlett in 2003.Recommanded Product: 86069-86-5 The following contents are mentioned in the article:

The synthesis of 2,3,5-triketopiperadines, e.g. I, on solid-support has been achieved for the first time. Cyclization using oxalyl diimidazole proceeded excellently with N-Me amino acids except for Sarcosine (Sar). On the other hand, this cyclization did not proceed well when amino acids without N-Me substitution were used. This can be explained by the lower energy difference between the trans and cis configurations of oxalyl amides by the introduction of N-Me substitution, because cis conformation is necessary for the cyclization to proceed. This cyclization also worked well with amino acids with a six-membered ring such as tetrahydroisoquinoline-3-carboxylic acid (Tic) and piperidine-2-carboxylic acid (Pic), which are N-alkylated amino acids. Although the purity of the target compounds was found to be low in the case of Sar and amino acids with a five-membered ring such as proline (Pro) and thiazolidine-4-carboxylic acid (Thz) under the same cyclization conditions, we were able to successfully optimize the reaction conditions to give the target compounds with good purity. Furthermore, it was demonstrated that 2,3,5-triketopiperadines with three points of diversity could be prepared on solid-support with high purity, showing the generality of this method. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Recommanded Product: 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Recommanded Product: 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Solid-phase synthesis of 2,3,5-triketopiperadine was written by Makino, Shingo;Nakanishi, Eiji;Tsuji, Takashi. And the article was included in Synlett in 2003.Synthetic Route of C21H21NO4 The following contents are mentioned in the article:

The synthesis of 2,3,5-triketopiperadines, e.g. I, on solid-support has been achieved for the first time. Cyclization using oxalyl diimidazole proceeded excellently with N-Me amino acids except for Sarcosine (Sar). On the other hand, this cyclization did not proceed well when amino acids without N-Me substitution were used. This can be explained by the lower energy difference between the trans and cis configurations of oxalyl amides by the introduction of N-Me substitution, because cis conformation is necessary for the cyclization to proceed. This cyclization also worked well with amino acids with a six-membered ring such as tetrahydroisoquinoline-3-carboxylic acid (Tic) and piperidine-2-carboxylic acid (Pic), which are N-alkylated amino acids. Although the purity of the target compounds was found to be low in the case of Sar and amino acids with a five-membered ring such as proline (Pro) and thiazolidine-4-carboxylic acid (Thz) under the same cyclization conditions, we were able to successfully optimize the reaction conditions to give the target compounds with good purity. Furthermore, it was demonstrated that 2,3,5-triketopiperadines with three points of diversity could be prepared on solid-support with high purity, showing the generality of this method. 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 metabolite of cadaverine, a polyamine found in the human intestine. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Synthetic Route of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Effect of soluble epoxide hydrolase polymorphism on substrate and inhibitor selectivity and dimer formation was written by Morisseau, Christophe;Wecksler, Aaron T.;Deng, Catherine;Dong, Hua;Yang, Jun;Lee, Kin Sing S.;Kodani, Sean D.;Hammock, Bruce D.. And the article was included in Journal of Lipid Research in 2014.Recommanded Product: 1222780-33-7 The following contents are mentioned in the article:

Epoxy FAs (EpFAs) are important lipid mediators that are mainly metabolized by soluble epoxide hydrolase (sEH). Thus, sEH inhibition is a promising therapeutic target to treat numerous ailments. Several sEH polymorphisms result in amino acid substitutions and alter enzyme activity. K55R and R287Q are associated with inflammatory, cardiovascular, and metabolic diseases. R287Q seems to affect sEH activity through reducing formation of a catalytically active dimer. Thus, understanding how these SNPs affect the selectivity of sEH for substrates and inhibitors is of potential clin. importance. We investigated the selectivity of four sEH SNPs toward a series of EpFAs and inhibitors. We found that the SNPs alter the catalytic activity of the enzyme but do not alter the relative substrate and inhibitor selectivity. We also determined their dimer/monomer constants (KD/M). The WT sEH formed a very tight dimer, with a KD/M in the low picomolar range. Only R287Q resulted in a large change of the KD/M. However, human tissue concentrations of sEH suggest that it is always in its dimer form independently of the SNP. These results suggest that the different biologies associated with K55R and R287Q are not explained by alteration in dimer formation or substrate selectivity. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Recommanded Product: 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Computed Properties of C21H21NO4 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Computed Properties of C21H21NO4).

(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 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Computed Properties of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Design and Combinatorial Development of Shield-1 Peptide Mimetics Binding to Destabilized FKBP12 was written by Madsen, Daniel;Joergensen, Frederik P.;Palmer, Daniel;Roux, Milena E.;Olsen, Jakob V.;Bols, Mikael;Schoffelen, Sanne;Diness, Frederik;Meldal, Morten. And the article was included in ACS Combinatorial Science in 2020.Application of 86069-86-5 The following contents are mentioned in the article:

The destabilizing domain (DD) is a double point-mutated version of the human protein FKBP12, and it has proven its vast utility in several biol. systems, where the level of a fused protein-of-interest may be controlled by the addition of the stabilizing small mol. Shield-1 (Shld1). With the aim of developing small peptide derived ligands that mimic the Shld1-DD interaction, we here report the synthesis and screening of a one-bead one-compound library consisting of triazole containing tripeptides. The library of peptide mimetics was synthesized on MicroParticle Matrix encoded PEGA1900 beads and deconvoluted using a decoder apparatus Verification of the hit’s activities was performed using an on-bead binding assay, where the binding profile of the immobilized substrates were correlated to a solid-supported version of the known SLF* ligand. These studies guided the design of small peptide-like compounds, which were readily synthesized in solution or on solid-support. The binding affinity of these focused peptide libraries towards the DD was tested using a competitive fluorescence polarization assay, which led to the discovery of peptide-ligands with low micromolar binding affinity. 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. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Application of 86069-86-5

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Protective effects of the soluble epoxide hydrolase inhibitor 1- trifluoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea in a rat model of permanent middle cerebral artery occlusion was written by Zhang, Linlei;Xu, Shasha;Wu, Xiaoxiao;Muse, Farah Mohamed;Chen, Jiaou;Cao, Yungang;Yan, Jueyue;Cheng, Zicheng;Yi, Xingyang;Han, Zhao. And the article was included in Frontiers in Pharmacology in 2020.Related Products of 1222780-33-7 The following contents are mentioned in the article:

Acute ischemic stroke is a serious disease that endangers human health. In our efforts to develop an effective therapy, we previously showed that the potent, highly selective inhibitor of soluble epoxide hydrolase called 1-trifuoromethoxyphenyl-3-(1- propionylpiperidin-4-yl) urea (TPPU) protects the brain against focal ischemia in rats. Here we explored the mechanism of TPPU action by assessing whether it could preserve blood-brain barrier integrity and reduce apoptosis in the brain during permanent middle cerebral artery occlusion in male Sprague-Dawley rats. TPPU administration at the onset of stroke and once daily thereafter led to smaller infarct volume and brain edema as well as milder neurol. deficits. TPPU significantly inhibited the activity of soluble epoxide hydrolase and matrix metalloproteases 2 and 9, reducing 14,15-DHET levels, while increasing expression of tight junction proteins. TPPU decreased numbers of apoptotic cells by down-regulating the pro-apoptotic proteins BAX and Caspase-3, while upregulating the anti-apoptotic protein BCL-2. Our results suggest that TPPU can protect the blood-brain barrier and reduce the apoptosis of brain tissue caused by ischemia. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7Related Products of 1222780-33-7).

1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7) 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. Piperidine prefers a chair conformation, similar to cyclohexane. Unlike cyclohexane, piperidine has two distinguishable chair conformations: one with the N鈥揌 bond in an axial position, and the other in an equatorial position.Related Products of 1222780-33-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Natural soluble epoxide hydrolase inhibitors from Inula helenium and their interactions with soluble epoxide hydrolase was written by He, Xin;Zhao, Wen-Yu;Shao, Bo;Zhang, Bao-Jing;Liu, Tian-Tian;Sun, Cheng-Peng;Huang, Hui-Lian;Wu, Jia-Rong;Liang, Jia-Hao;Ma, Xiao-Chi. And the article was included in International Journal of Biological Macromolecules in 2020.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea The following contents are mentioned in the article:

The inhibition of soluble epoxide hydrolase (sEH) is regarded as a promising therapeutic approach to treat inflammation and its related disorders. In present work, we investigated inhibitory effects of forty-nine kinds of traditional Chinese medicines against sEH. Inula helenium showed significant inhibitory effect against sEH, and the extract of I. helenium was isolated to obtain eight compounds, including 4H-tomentosin (1), xanthalongin (2), linoleic acid (3), 8-hydroxy-9-isobutyryloxy-10(2)-methylbutyrylthymol (4), dehydrocostus lactone (5), alantolactone (6), costunolide (7), and isoalantolactone (8). Among them, 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) showed significantly inhibitory activities on sEH with half maximal inhibitory concentration (IC₅₀) from 5.88 卤 0.97渭M to 11.63 卤 0.58渭M. The inhibition kinetics suggested that 4H-tomentosin (1) and xanthalongin (2) were mixed-competitive type inhibitors with inhibition constants (K_i) of 7.02 and 6.57渭 M, resp., and linoleic acid (3) was a competitive type inhibitor with a K_i values of 3.52渭M. The potential interactions of 4H-tomentosin (1), xanthalongin (2), and linoleic acid (3) with sEH were analyzed by mol. docking, which indicated that these bioactive compounds had interactions with key amino acid residues Tyr343, Ile363, Tyr383, and His524. 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 is a metabolite of cadaverine, a polyamine found in the human intestine. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Novel cinchona carbamate selectors with complementary enantioseparation characteristics for N-acylated amino acids was written by Krawinkler, Karl Heinz;Maier, Norbert M.;Ungaro, Rocco;Sansone, Francesco;Casnati, Alessandro;Lindner, Wolfgang. And the article was included in Chirality in 2003.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

The synthesis and chromatog. evaluation of the enantiomer separation capabilities of covalently immobilized calix[4]arene-cinchona carbamate hybrid type receptors derived from quinine (QN) and its corresponding C9-epimer (eQN) in different solvents are reported. The receptors display complementary enantiomer separation profiles in terms of elution order, chiral substrate specificity, and mobile phase characteristics, indicating the existence of two distinct chiral recognition mechanisms. The QN-derived receptor binds the (S)-enantiomers of N-acylated amino acids more strongly, shows preferential recognition of open-chained amino acids, and superior enantioselectivity in polar media such as methanol/acetic acid. In contrast, the eQN congener preferentially recognizes the corresponding (R)-enantiomers, displays good enantioselectivity (伪 up to 1.74) for cyclic amino acids, and enhanced stereodiscriminating properties in apolar mobile phases, e.g., chloroform/acetic acid. A comparison of the enantiomer separation profiles with those of the corresponding QN and eQN tert-Bu carbamate congeners indicates no significant level of cooperativity between the calix[4]arene module and the cinchona units in terms of overall chiral recognition, most probably as a consequence of residual conformational flexibility of the calixarene module and the carbamate linkage. 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 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Novel cinchona carbamate selectors with complementary enantioseparation characteristics for N-acylated amino acids was written by Krawinkler, Karl Heinz;Maier, Norbert M.;Ungaro, Rocco;Sansone, Francesco;Casnati, Alessandro;Lindner, Wolfgang. And the article was included in Chirality in 2003.Category: piperidines The following contents are mentioned in the article:

The synthesis and chromatog. evaluation of the enantiomer separation capabilities of covalently immobilized calix[4]arene-cinchona carbamate hybrid type receptors derived from quinine (QN) and its corresponding C9-epimer (eQN) in different solvents are reported. The receptors display complementary enantiomer separation profiles in terms of elution order, chiral substrate specificity, and mobile phase characteristics, indicating the existence of two distinct chiral recognition mechanisms. The QN-derived receptor binds the (S)-enantiomers of N-acylated amino acids more strongly, shows preferential recognition of open-chained amino acids, and superior enantioselectivity in polar media such as methanol/acetic acid. In contrast, the eQN congener preferentially recognizes the corresponding (R)-enantiomers, displays good enantioselectivity (伪 up to 1.74) for cyclic amino acids, and enhanced stereodiscriminating properties in apolar mobile phases, e.g., chloroform/acetic acid. A comparison of the enantiomer separation profiles with those of the corresponding QN and eQN tert-Bu carbamate congeners indicates no significant level of cooperativity between the calix[4]arene module and the cinchona units in terms of overall chiral recognition, most probably as a consequence of residual conformational flexibility of the calixarene module and the carbamate linkage. 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. 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. 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.Category: piperidines

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem