934369-14-9|TY-52156|CsnPharm

CAS No.: 934369-14-9

TY-52156 Catalog No. CSN18599

Synonyms: Ty-52156

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.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Sphingosine 1-phosphate (S1P) induces diverse biological responses in various tissues by activating specific G protein-coupled receptors (S1P₁–S1P₅ receptors) ^[2]. TY-52156 is a potent and selective S1P₃ receptor antagonist with a K_i value of 110 nM. In functional studies, TY-52156 showed submicromolar potency and a high degree of selectivity for S1P₃ receptor. Effect of TY-52156 on both the S1P-induced increase in intracellular calcium ([Ca²⁺]_i) and Rho activation that are responsible for the contraction of human coronary artery smooth muscle cells had been investigated. TY-52156 inhibited both the S1P-induced increase in [Ca²⁺]_i and Rho activation ^[2]. TY-52156 inhibited FTY-720-induced S1P₃ receptor-mediated bradycardia in vivo. These results clearly show that 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 ^[2].
参考文献

[1] Murakami A, Takasugi H, 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.
[2] Murakami A, Takasugi H, Ohnuma S, Koide Y, Sakurai A, Takeda S, Hasegawa T, Sasamori J, Konno T, Hayashi K, Watanabe Y, Mori K, Sato Y, Takahashi A, Mochizuki N, Takakura N. 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. doi: 10.1124/mol.109.061481. Epub 2010 Jan 22. PMID: 20097776.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7452 mL
- 13.7261 mL
- 27.4522 mL
- 5 mM
- 0.5490 mL
- 2.7452 mL
- 5.4904 mL
- 10 mM
- 0.2745 mL
- 1.3726 mL
- 2.7452 mL

技术信息

CAS号

934369-14-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H19Cl2N3O

运输

蓝冰

分子量

364.27

别名

Ty-52156

溶解度

DMSO	100.0 mg/mL (274.5 mM)
Water	Insoluble

动物实验配方

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