1586787-08-7
Chemical Structure
CMF019
- CAS No.: 1586787-08-7
- Formula:C25H33N3O3S
- Molecular Weight:455.61
IUPAC Name: (S)-5-methyl-3-(1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido)hexanoic acid
InChIKey: VCQKKZXFASLXAH-SFHVURJKSA-N
SMILES: CC(C)C[C@H](NC(C1=CC=C2C(N=C(CC3=CC=CS3)N2C(CC)CC)=C1)=O)CC(O)=O
Biological Activity: CMF019 is an orally active, 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. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension[1][2][3][4].
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CMF019 | 99.89% | CMF019 is an orally active, 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. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension. | ||||||||||||||||||||
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CMF019 (Standard) | ≥98% | CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. CMF019 is an orally active, 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. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
- [3]. Ma K F O, et al. CMF-019 elevates neuronal insulin sensitivity: an implication of therapeutic potential of Alzheimer’s disease[C]//26th Medical Research Conference. Hong Kong Academy of Medicine Press. The Journal's web site is located at http://www. hkmj. org/, 2021.
- [4]. Read C, et al. The G Protein Biased Small Molecule Apelin Agonist CMF-019 is Disease Modifying in Endothelial Cell Apoptosis In Vitro and Induces Vasodilatation Without Desensitisation In Vivo. Front Pharmacol. 2021 Jan 21;11:588669. [Content Brief]
Keywords
