Apelin Receptor (APJ) Antagonist

ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC₈₀ of 10 nM in both assays.

ML339 is a selective CXCR6 antagonist with an IC₅₀ of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC₅₀ of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC₅₀ of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC₅₀ >79 μM. ML339 has the potential to promote the development of prostate cancer research.

YL-GB063 is an Apelin receptor (APJ) antagonist. YL-GB063 inhibits Apelin-induced APJ β-arrestin recruitment (IC₅₀ of 3.1 μM in HTLA cells). YL-GB063 has anti-cancer activity against ovarian cancer.

(Ala13)-Apelin-13 TFA is a potent apelin receptors (APJ) antagonist. (Ala13)-Apelin-13 TFA inhibits gastric motility through vagal cholinergic pathway.

APJ antagonist-1 is an apelin receptor (APJ) antagonist. APJ antagonist-1 shows strong β-arrestin inhibition with an IC₅₀ of 3.1 μM. APJ antagonist-1 selectively inhibits APJ-overexpressing cancer cells and suppresses apelin-induced endothelial cell migration. APJ antagonist-1exhibits high metabolic stability. APJ antagonist-1 can used for the studies of ovarian cancer and tumor angiogenesis.

(Ala13)-Apelin-13 is a potent apelin receptors (APJ) antagonist. (Ala13)-Apelin-13 inhibits gastric motility through vagal cholinergic pathway.

ML221 (Standard) is the analytical standard of ML221 (HY-103254). This product is intended for research and analytical applications. ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.