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MedChemExpressModel CMF019 -1586787-08-7

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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

MCE China:CMF019

Brand:MedChemExpress (MCE)

Cat. No.HY-103080

CAS:1586787-08-7

Purity:99.89%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

In Vitro:CMF019 (1-10 μM, 18 h) rescues human pulmonary arterial endothelial cells (PAEC) apoptosis induced by TNFα and CHX [4].

In Vivo:CMF019 (50-5000 nmol, 0.5 mL, i.v., three successive doses) reduces peripheral artery pressure in rats[4].

IC50 & Target:pKi: 8.58 (human Apelin receptor) ; 8.49 (rat Apelin receptor); 8.71 (mouse Apelin receptor)[1]. Cellular Effect Cell Line Type Value Description References

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References:

[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]

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