TY-52156
产品说明书
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同义名 : | - |
| CAS号 : | 934369-14-9 | |
| 货号 : | A429860 | |
| 分子式 : | C18H19Cl2N3O | |
| 纯度 : | 99%+ | |
| 分子量 : | 364.269 | |
| MDL号 : | MFCD28396419 | |
| 存储条件： |
Pure form Keep in dark place, sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(288.25 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 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 Ki 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]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.75mL 0.55mL 0.27mL |
13.73mL 2.75mL 1.37mL |
27.45mL 5.49mL 2.75mL |
| 参考文献 |
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