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 TGFβ pathway, priming hESCs toward the endoderm lineage. Stimulates angiogenesis in HUVEC cells. Relaxes mouse aortic vessels. Functions as an anorexigenic hormone through activation of the AVP and CRH neurons in the PVN.

The herbs of Leonurus artemisia.

S961 TFA is A high affinity insulin receptor (IR) antagonist with IC50 for hir-a, hir-b and human insulin-like growth factor I receptor (higf-ir) at 0.048, 0.027 and 630 nM, respectively.