For research use only. Not for therapeutic Use.
CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents[1]. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin[2].
| Catalog Number | I017997 |
| CAS Number | 1586787-08-7 |
| Synonyms | (3S)-5-methyl-3-[[1-pentan-3-yl-2-(thiophen-2-ylmethyl)benzimidazole-5-carbonyl]amino]hexanoic acid |
| Molecular Formula | C25H33N3O3S |
| Purity | ≥95% |
| InChI | InChI=1S/C25H33N3O3S/c1-5-19(6-2)28-22-10-9-17(25(31)26-18(12-16(3)4)14-24(29)30)13-21(22)27-23(28)15-20-8-7-11-32-20/h7-11,13,16,18-19H,5-6,12,14-15H2,1-4H3,(H,26,31)(H,29,30)/t18-/m0/s1 |
| InChIKey | VCQKKZXFASLXAH-SFHVURJKSA-N |
| SMILES | CCC(CC)N1C2=C(C=C(C=C2)C(=O)NC(CC(C)C)CC(=O)O)N=C1CC3=CC=CS3 |
| Reference | [1]. Trifonov L, et al. An Expedient Synthesis of CMF-019: (S)-5-Methyl-3-{1-(pentan-3-yl)-2- (thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido}hexanoic Acid, a Potent Apelin Receptor (APJ) Agonist. Med Chem. 2018;14(7):688-694. [2]. Read C, et al. Cardiac action of the first G protein biased small molecule apelin agonist. Biochem Pharmacol. 2016 Sep 15;116:63-72. |
