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Chemical Structure : CMF-019
CAS No.: 1586787-08-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 455.617 | |
| Formula | C25H33N3O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-5-Methyl-3-(1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido)hexanoic acid |
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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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