TY-52156

TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor.IC50 value: 110 nM (Ki)Target: S1P3in vitro: TY-52156 shows submicromolar potency and a high degree of selectivity for S1P3 receptor. TY-52156 is both sensitive and useful as an S1P3 receptor-specific antagonist and reveal that S1P induces vasoconstriction by directly activating S1P3 receptor and through a subsequent increase in [Ca2+]i and Rho activation in vascular smooth muscle cells. TY-52156 has a selective antagonistic effect toward S1P3 receptor. [1]in vivo: TY-52156 Suppresses S1P3 Receptor-Induced Bradycardia In Vivo. the oral administration of TY-52156 inhibits S1P3 receptor-dependent bradycardia. [1]

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

Research Areas >> Cardiovascular Disease

[1]. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13.

Ki16425 | Siponimod | AM966 | Ozanimod | BMS-986020 | LPA2 antagonist 1 | AM095 | Etrasimod | ACT-334441 | Ponesimod | Amiselimod hydrochloride | S1p receptor agonist 1 | ONO-7300243 | (S) FTY720 Phosphate