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首页-小分子抑制剂&激动剂-GPCR-Apelin Receptor (APLNR)-CMF-019
CMF-019

Chemical Structure : CMF-019

CAS No.: 1586787-08-7

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CMF-019 (CMF019)

货号: PC-38139Not For Human Use, Lab Use Only.

CMF-019 (CMF019) is the first G protein biased small molecule Apelin receptor (APJ, APLNR) agonist, potent benzimidazole-derived apelin peptidomimetic, binds to APLNR with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse APLNR, respectively.

规格 价格 库存 数量
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CMF-019 (CMF019) is the first G protein biased small molecule Apelin receptor (APJ, APLNR) agonist, potent benzimidazole-derived apelin peptidomimetic, binds to APLNR with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse APLNR, respectively.
CMF-019 caused dose-dependent vasodilatation in vivo, rescues human pulmonary artery endothelial cells from apoptosis induced by tumor necrosis factor α and cycloheximide.
CMF-019 displays remarkable bias at the apelin receptor, recapitulates all aspects of the cardiovascular responses to the endogenous ligand, [Pyr1]apelin-13, in vivo.
CMF-019 is suitable as a tool compound and provides the basis for design of biased agonists with improved pharmacokinetics for treatment of cardiovascular conditions such as pulmonary arterial hypertension.

物理化学性质&存储条件

分子量 455.617
分子式 C25H33N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 1 Month
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-5-Methyl-3-(1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido)hexanoic acid

参考文献

1. Lena Trifonov, et al. Med Chem. 2018;14(7):688-694.

2. U.S. Patent 2014,0094450 Al, April 3,2014

3. Read C, et al. Biochem Pharmacol. 2016 Sep 15;116:63-72. 

4. Read C, et al. Front Pharmacol. 2021 Jan 21;11:588669.

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