|4-(4-氟萘-1-基)-6-异丙基嘧啶-2-胺|CsnPharm

CAS No.: 199864-87-4

RS-127445 Catalog No. CSN13491

Synonyms: MT500

RS 127445 is a potent and selective antagonist at 5-HT2B receptor with pKi value of 9.5.

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生物活性

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技术信息

生物活性

描述RS-127445, a selective, high anity, orally bioavailable 5-HT2B receptor antagonist. RS-127445 potently displaced [3H]-5-HT from human recombinant 5-HT2B receptor expressed in CHO-K1 cells. The anity (pKi value) of RS-127445 for the 5-HT2B receptor was 9.5+0.1. In vitro research suggests RS-127445 potently inhibited the 5-HT evoked increase in the formation of inositol phosphates in cells expressing 5-HT2B receptor. RS-127445 potently blocked the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK293 cells expressing the 5-HT2B receptor (pIC50 value of 10.4+0.1). RS-127445 potently blocked the 5-HT evoked contraction of the isolated fundus. Peak plasma concentrations were rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration^[3].
参考文献

[1] Ohashi-Doi K, Himaki D, et al. A selective, high affinity 5-HT 2B receptor antagonist inhibits visceral hypersensitivity in rats. Neurogastroenterol Motil. 2010 Feb;22(2):e69-76.
[2] Bonhaus DW, Flippin LA, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82.
[3] Bonhaus DW, Flippin LA, Greenhouse RJ, Jaime S, Rocha C, Dawson M, Van Natta K, Chang LK, Pulido-Rios T, Webber A, Leung E, Eglen RM, Martin GR. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82. doi: 10.1038/sj.bjp.0702632. PMID: 10455251; PMCID: PMC1566110.

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
- 3.5546 mL
- 17.7729 mL
- 35.5458 mL
- 5 mM
- 0.7109 mL
- 3.5546 mL
- 7.1092 mL
- 10 mM
- 0.3555 mL
- 1.7773 mL
- 3.5546 mL

技术信息

CAS号

199864-87-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H16FN3

运输

蓝冰

分子量

281.33

别名

MT500

溶解度

DMSO	255.0 mg/mL (906.4 mM)
Water	insoluble

动物实验配方

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