TY 52156

Short Summary : sphingosine-1-phosphate receptor 3 (SIP3) antagonist

Category : GPCR/G protein|S1P receptor inhibitor

Purity : 0.98

CAS Number : 934369-14-9

Formula : C18H19Cl2N3O

Molecular Weight :

Molecular Weight : 364.3

SMILE : CC(C)(C)C(/C(NNC1=CC=C(Cl)C=C1)=N/C2=CC=C(Cl)C=C2)=O

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : TY 52156 (1-(4-chlorophenylhydrazono)-1-(4-chlorophenylamino)-3,3-dimethyl-2-butanone) is a novel S1P3 receptor antagonist [1]. Sphingosine 1-phosphate (S1P) is a bioactive lysophospholipid mediator mainly released from activated platelets and implicated in many biological responses, such as angiogenesis, vascular development, and cardiovascular function [1].In vitro: TY-52156 preferentially inhibited the S1P-induced increase in [Ca2+]i in S1P3-CHO cells. TY-52156 competitively inhibited the dose-dependent [Ca2+]i increase elicited by S1P in S1P3-CHO with the Ki value of 110 nM for S1P3 receptor. TY-52156 showed submicromolar potency and a high degree of selectivity for S1P3 receptor. TY-52156 (10 M) inhihbited 24 GPCRs and three ion channels by 30%. S1P dose-dependently decreased CF (Coronary Flow) in perfused rat heart. S1P dose-dependently induced vasoconstriction in isolated canine cerebral arteries. In HCASMCs, TY-52156 inhibited S1P-induced Rho activation.In vivo: in SD rats, oral bioavailability of TY-52156 was 70.9%. In rats, pretreatment with TY-52156 significantly attenuated FTY-720-induced bradycardia, a broad agonist of S1P receptors. Pretreatment with TY-52156 prevented the FTY-720-P-induced increase in [Ca2+]i in a dose-dependent manner.Reference:[1] Murakami A, Takasugi H, Ohnuma S, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist[J]. Molecular pharmacology, 2010, 77(4): 704-713.

Download datasheet