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TY-52156

  Cat. No.:  DC24077   Featured
Chemical Structure
934369-14-9
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More than 5000 active chemicals with high quality for research!
Field of application
TY-52156 is a potent and selective inhibitor of S1P3 receptor (Ki=110 nM).
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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