CMF019

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].

Product Specifications

CAS Number

[1586787-08-7]

UNSPSC

12352005

Target

Apelin Receptor (APJ)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/cmf019.html

Purity

99.89

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC(C)C[C@H](NC(C1=CC=C2C(N=C(CC3=CC=CS3)N2C(CC)CC)=C1)=O)CC(O)=O

Molecular Formula

C25H33N3O3S

Molecular Weight

455.61

References & Citations

[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.|[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.