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TY 52156
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TY 52156图片
CAS NO:934369-14-9
规格:98%
分子量:364.3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
sphingosine-1-phosphate receptor 3 (SIP3) antagonist
CAS:934369-14-9
分子式:C18H19Cl2N3O
分子量:364.3
纯度:98%
存储:Store at -20°C

Background:

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 μM) 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.