Month: November 2022

Influence of the Trans/Cis Conformer Ratio on the Stereoselectivity of Peptidic Catalysts was written by Schnitzer, Tobias;Wennemers, Helma. And the article was included in Journal of the American Chemical Society in 2017.Electric Literature of C21H21NO4 The following contents are mentioned in the article:

Trans/cis isomerization of Xaa-Pro bonds is key for the structure and function of several enzymes. In recent years, numerous versatile peptidic catalysts have been developed that bear Xaa-Pro amide bonds. Due to the many degrees of freedom within even short peptides, the design and optimization of peptidic catalysts by rational structural modifications is difficult. We envisioned that control over the trans/cis amide bond ratio may provide a tool to optimize the catalytic performance of peptidic catalysts. Here, we investigated the influence of the amide bond conformation on the stereoselectivity of H-Pro-Pro-Xaa-NH₂-type peptidic catalysts in conjugate addition reactions. The middle Pro residue within the tripeptides was replaced with analogs of varying ring sizes (azetidine carboxylic acid, Aze, and piperidine carboxylic acid, Pip) to produce different trans/cis ratios in different solvents. The studies revealed a direct correlation between the trans/cis amide bond ratio and the enantio- and diastereoselectivity of structurally related peptidic catalysts. These insights led to the identification of H-D-Pro-Pip-Glu-NH₂ as a highly reactive and stereoselective amine-based catalyst that allows C-C bond formations to be performed in the presence of as little as 0.05 mol %, which is the lowest catalyst loading yet achieved for organocatalyzed reactions that rely on an enamine-based mechanism. 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 and its derivatives have become increasingly popular in many synthetic schemes. 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.Electric Literature of C21H21NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Intestinal absorption of alogliptin is mediated by a fruit-juice-sensitive transporter was written by Morimoto, Kaori;Sasaki, Momona;Oikawa, Erika;Abe, Maho;Kikuchi, Tatsuro;Ishii, Makoto;Ogihara, Takuo;Tomita, Mikio. And the article was included in Biological & Pharmaceutical Bulletin in 2021.Computed Properties of C32H39NO4 The following contents are mentioned in the article:

Alogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP = -1.4). Here, we aimed to clarify the mechanism of its intestinal absorption. The ALG uptake into Caco-2 cells was time-, temperature-, and concentration-dependent, but was not saturated at concentrations up to 10 mmol/L. The uptake was significantly inhibited by the organic anion transporting polypeptide (OATP) substrate fexofenadine and by the OATP inhibitor 4,4′-diisothiocyanostilbene-2,2′-disulfonic acid (DIDS), but was not inhibited by organic cation transporter (OCT)/organic cation/carnitine transporter (OCTN) or peptide transporter 1 (PEPT1) substrates. Grapefruit, orange, and apple juices and their constituents, which are known to strongly inhibit intestinal OATPs, significantly inhibited ALG uptake into Caco-2 cells. The pH dependence was bell-shaped, indicating the involvement of a pH-sensitive transporter. However, ALG uptake by HEK293 cells overexpressing OATP2B1, a key intestinal OATP transporter of amphiphilic drugs, was not different from that of mock cells. In a rat in vivo study, apple juice reduced systemic exposure to orally administered ALG without changing the terminal half-life. These observations suggest that intestinal absorption of ALG is carrier-mediated, and involves a fruit-juice-sensitive transporter other than OATP2B1. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Computed Properties of C32H39NO4).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. 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.Computed Properties of C32H39NO4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Designing hybrid barium tungstate on functionalized carbon black as electrode modifier for low potential detection of antihistamine drug promethazine hydrochloride was written by Muthukutty, Balamurugan;Vivekanandan, Alangadu Kothandan;Chen, Shen-Ming;Sivakumar, Mani;Chen, Shih-Hsun. And the article was included in Composites, Part B: Engineering in 2021.Product Details of 83799-24-0 The following contents are mentioned in the article:

Promethazine hydrochloride (PMHC) is a first-generation antihistamine drug used to treat allergic rhinitis, allergic conjunctivitis, urticaria, etc. Overdosage of PMHC affects majorly the central nervous system such as respiratory tract, dermatol., cardiovascular and hematol. Hence, the detection of PMHC considered being an important factor in day to day life of the human. In this work, we developed barium tungstate (BaWO₄) unified with functionalized carbon black (f-CB) via an eco-friendly synthesis technique to detect PMHC. As prepared BaWO₄/f-CB composite was analyzed through various spectroscopic and microscopic techniques. The electrochem. property of the as-prepared composite was investigated through electron impedance spectroscopy (EIS), and voltammetric techniques with a disposable screen-printed carbon electrode (SPCE) as a working electrode. BaWO₄/f-CB/SPCE outcomes with least charge resistance, higher anodic current, dual wider linear range, lower limit of detection (29 nM) Å limit of quantification (264 nM), excellent sensitivity, and selectivity towards PMHC. Addnl., the PMHC concentration in pharmaceutical formulations (medical wastes) largely pollutes the hydric resources. Hence, the lake water was chosen to analyze the practical feasibility of a proposed sensor. The practical utility of BaWO₄/f-CB sensor fallout with good electrocatalytic activity at trace level detection of PMHC. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Product Details of 83799-24-0).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) 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 α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Product Details of 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

An automated methodology for non-targeted compositional analysis of small molecules in high complexity environmental matrices using coupled ultra performance liquid chromatography orbitrap mass spectrometry was written by Pereira, Kelly L.;Ward, Martyn W.;Wilkinson, John L.;Sallach, Jonathan Brett;Bryant, Daniel J.;Dixon, William J.;Hamilton, Jacqueline F.;Lewis, Alastair C.. And the article was included in Environmental Science & Technology in 2021.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

The life-critical matrixes of air and water are among the most complex chem. mixtures that are ever encountered. Ultrahigh-resolution mass spectrometers, such as the Orbitrap, provide unprecedented anal. capabilities to probe the mol. composition of such matrixes, but the extraction of non-targeted chem. information is impractical to perform via manual data processing. Automated non-targeted tools rapidly extract the chem. information of all detected compounds within a sample dataset. However, these methods have not been exploited in the environmental sciences. Here, we provide an automated and (for the first time) rigorously tested methodol. for the non-targeted compositional anal. of environmental matrixes using coupled liquid chromatog.-mass spectrometric data. First, the robustness and reproducibility was tested using authentic standards, evaluating performance as a function of concentration, ionization potential, and sample complexity. The method was then used for the compositional anal. of particulate matter and surface waters collected from worldwide locations. The method detected >9600 compounds in the individual environmental samples, arising from critical pollutant sources, including carcinogenic industrial chems., pesticides, and pharmaceuticals among others. This methodol. offers considerable advances in the environmental sciences, providing a more complete assessment of sample compositions while significantly increasing throughput. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Mechanisms of Regulation of the P-Glycoprotein Transporter Protein Functioning under the Action of Nitric Oxide was written by Shchulkin, Aleksey V.;Abalenikhina, Yulia V.;Sudakova, Elena A.;Mylnikov, Pavel Yu.;Yakusheva, Elena N.. And the article was included in Biochemistry (Moscow) in 2022.SDS of cas: 83799-24-0 The following contents are mentioned in the article:

Mechanisms of regulation of the P-glycoprotein (Pgp) transporter under the action of nitric oxide (NO) were studied in Caco-2 cells. S-Nitrosoglutathione (GSNO) was used as a NO donor, which was added to the cells at concentrations 1, 10, 50, 100, and 500μM and incubated for 3, 24, or 72 h. The amount of Pgp was analyzed using Western blotting, activity was determined by monitoring transport of its substrate, fexofenadine. The study showed that a short-term exposure to GSNO for 3 h at 500μM concentration caused increase in the concentration of peroxynitrite in Caco-2 cells, which reduced the activity, but not the amount of Pgp. Increase in the duration of exposure to 24 h increased the amount and activity of Pgp at GSNO concentrations of 10 and 50μM, increased the amount without increasing activity at 100μM concentration, and decreased the amount of the transporter protein at 500μM. Duration of exposure to GSNO of 72 h at concentration of 10μM resulted in the increase of the amount and activity of Pgp, while at concentration of 100 and 500μM it decreased the amount of the transport protein. At the same time, it was shown using specific inhibitors that the increase in the amount of Pgp under the influence of low concentrations of GSNO was realized through the NO-cGMP signaling pathway, and the effect of the higher concentration of GSNO and the resp. development of nitrosative stress was realized through Nrf2 and the constitutive androstane receptor. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0SDS of cas: 83799-24-0).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) 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 α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.SDS of cas: 83799-24-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Peripheral soluble epoxide hydrolase inhibition reduces hypernociception and inflammation in albumin-induced arthritis in temporomandibular joint of rats was written by Teixeira, Juliana Maia;Abdalla, Henrique Ballassini;Basting, Rosanna Tarkany;Hammock, Bruce D.;Napimoga, Marcelo Henrique;Clemente-Napimoga, Juliana Trindade. And the article was included in International Immunopharmacology in 2020.COA of Formula: C16H20F3N3O3 The following contents are mentioned in the article:

Rheumatoid arthritis (RA) is characterized by chronic inflammation of the synovial tissue, joint dysfunction, and damage. Epoxyeicosatrienoic acids (EETs) are endogenous anti-inflammatory compounds, which are quickly converted by the soluble epoxide hydrolase (sEH) enzyme into a less active form with decreased biol. effects. The inhibition of the sEH enzyme has been used as a strategy to lower nociception and inflammation. The goal of this study was to investigate whether the peripheral treatment with the sEH enzyme inhibitor 1- trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) could prevent the hypernociception and inflammation in the albumin-induced arthritis model in rats’ temporomandibular joint (TMJ). After the induction of exptl. arthritis, animals were assessed for nociceptive behavior test, leukocyte infiltration counts and histol. anal., ELISA to quantify several cytokines and Western blotting. The peripheral pretreatment with TPPU inhibited the arthritis-induced TMJ hypernociception and leukocyte migration. Moreover, the local concentrations of proinflammatory cytokines were diminished by TPPU, while the anti-inflammatory cytokine interleukin-10 was up-regulated in the TMJ tissue. Finally, TPPU significantly decreased protein expression of iNOS, while did not alter the expression of MRC1. This study provides evidence that the peripheral administration of TPPU reduces hypernociception and inflammation in TMJ exptl. arthritis. This study involved multiple reactions and reactants, such as 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea (cas: 1222780-33-7COA of Formula: C16H20F3N3O3).

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. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.COA of Formula: C16H20F3N3O3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A 3D microfluidic liver model for high throughput compound toxicity screening in the OrganoPlate was written by Bircsak, Kristin M.;DeBiasio, Richard;Miedel, Mark;Alsebahi, Alaa;Reddinger, Ryan;Saleh, Anthony;Shun, Tongying;Vernetti, Lawrence A.;Gough, Albert. And the article was included in Toxicology in 2021.Quality Control of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid The following contents are mentioned in the article:

We report development, automation and validation of 3D, microfluidic liver-on-a-chip for high throughput hepatotoxicity screening, OrganoPlate LiverTox. The model is comprised of aggregates of induced pluripotent stem cell-derived hepatocytes seeded in an extracellular matrix in organ channel and co-cultured with endothelial cells and THP-1 monoblasts differentiated to macrophages seeded in vascular channel of the 96 well Mimetas OrganoPlate 2-lane. A combination of secretome measurements and image-based anal. was used to demonstrate stable 15 day cell viability, albumin and urea secretion. Over same time-period, CYP3A4 activity increased and alpha-fetoprotein secretion decreased suggesting further maturation of iHeps. Troglitazone, clin. hepatotoxin, was chosen as control compound for validation studies. Albumin, urea, hepatocyte nuclear size and viability staining provided Robust Z’factors > 0.2 in plates treated 72 h with 180μM troglitazone compared with vehicle control. The viability assay provided the most robust statistic for a Robust Z’ factor = 0.6. A small library of 159 compounds with known liver effects was added to OrganoPlate LiverTox model for 72 h at 50μM and Toxicol. Prioritization scores were calculated A follow up dose-response evaluation of select hits revealed albumin assay to be most sensitive in calculating TC50 values. This platform provides a robust, novel model which can be used for high throughput hepatotoxicity screening. This study involved multiple reactions and reactants, such as 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0Quality Control of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid).

2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid (cas: 83799-24-0) 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.Quality Control of 2-(4-(1-Hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

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 33a–v. 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

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 33a–v. 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

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