mouse apelin receptor

CMF019 (CMF-019) is a potent, G-protein-biased small-molecule agonist of the Apelin receptor (APJ/APLNR). CMF019 exhibits pKi values of 8.58, 8.49, and 8.71 for binding to APJ in humans, rats, and mice, respectively. CMF-019 exhibits cardioprotective effects in rodents. CMF019 can be utilized in mechanism and drug development for heart failure and pulmonary arterial hypertension.

Apelin-36(rat, mouse) TFA, an endogenous agonist for the orphan G protein-coupled receptor APJ, exhibits a strong affinity for APJ receptors with an IC 50 of 5.4 nM and effectively inhibits cAMP production with an EC 50 of 0.52 nM. Moreover, it obstructs the invasion of certain HIV-1 and HIV-2 strains into NP-2/CD4 cells that express the APJ receptor [1] [2].

Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model

Potent, high affinity apelin receptor agonist (IC50 = 0.27 nM; Kd = 0.51 nM). Exhibits no binding GPR15 and GPR25. Activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. Also potentiates the T