TY-52156| CAS 934369-14-9|DC Chemicals

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

Description:	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.
Target:	IC50 value: 110 nM (Ki) Target: S1P3
In Vivo:	TY-52156 Suppresses S1P3 Receptor-Induced Bradycardia In Vivo. the oral administration of TY-52156 inhibits S1P3 receptor-dependent bradycardia. [1]
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]
References:	[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.

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