TY-52156 Datasheet | DC24077

TY-52156 — Datasheet

CAT. NO. DC24077

Parameter	Value
Chemical Name	Butanimidic acid, N-(4-chlorophenyl)-3,3-dimethyl-2-oxo-, 2-(4-chlorophenyl)hydrazide
CAS No.	934369-14-9
Synonyms	TY52156;TY 52156
Formula	C18H19Cl2N3O
M.Wt	364.269
SMILES	ClC1C=CC(N=C(C(=O)C(C)(C)C)NNC2C=CC(Cl)=CC=2)=CC=1
Purity	>98%
Storage	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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.

In 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]

Target

IC50 value: 110 nM (Ki) Target: S1P3

References & source

[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.

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.