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| | Hexanoic acid, 3-[[[1-(1-ethylpropyl)-2-(2-thienylmethyl)-1H-benzimidazol-5-yl]carbonyl]amino]-5-methyl-, (3S)- Basic information |
| | Hexanoic acid, 3-[[[1-(1-ethylpropyl)-2-(2-thienylmethyl)-1H-benzimidazol-5-yl]carbonyl]amino]-5-methyl-, (3S)- Chemical Properties |
| Boiling point | 703.3±55.0 °C(Predicted) | | density | 1.22±0.1 g/cm3(Predicted) | | pka | 4.16±0.10(Predicted) | | form | Solid | | color | White to light yellow |
| | Hexanoic acid, 3-[[[1-(1-ethylpropyl)-2-(2-thienylmethyl)-1H-benzimidazol-5-yl]carbonyl]amino]-5-methyl-, (3S)- Usage And Synthesis |
| Description | CMF-019 is a small molecule agonist with G protein bias. CMF-019 is the first potent biased small molecule identified at the apelin receptor and increases cardiac contractility in vivo. | | Uses | 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]. | | in vivo | CMF019 (50-5000 nmol, 0.5 mL, i.v., three successive doses) reduces peripheral artery pressure in rats[4].
| Animal Model: | male Sprague-Dawley rats[2] | | Dosage: | 50-5000 nmol, 0.5 mL | | Administration: | i.v., three successive doses | | Result: | Revealed reproducible peripheral reduction in femoral artery pressure. |
| | 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. DOI:10.2174/1573406414666180412154952
[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. DOI:10.1016/j.bcp.2016.07.018
[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. DOI:10.3389/fphar.2020.588669 |
| | Hexanoic acid, 3-[[[1-(1-ethylpropyl)-2-(2-thienylmethyl)-1H-benzimidazol-5-yl]carbonyl]amino]-5-methyl-, (3S)- Preparation Products And Raw materials |
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