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MedChemExpress - Model CMF019 -1586787-08-7
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].MCE products for research use only. We do not sell to patients.
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]
[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]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world;
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas;
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects;
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services;
• It has a professional experimental center and strict quality control and verification system;
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products;
• The biological activity of the products has been verified by the experiments of customers in various countries;
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers;
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world;
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。
