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RS127445

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产品信息

产品名称：RS127445	纯度：99% min
CAS NO：199864-87-4	溶解度：DMSO : ≥ 31 mg/mL (97.55 mM)
分子式：C₁₇H₁₇ClFN₃	包装：可按客户要求包装。
分子量：317.788	贮存：-20℃

质量控制

备注说明

RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3).

中文名称：

4-(4-氟-1-萘)-6-(1-甲基乙基)-2-嘧啶胺盐酸盐

物化属性:

密度：1.213

沸点：472.8°C at 760 mmHg

折射率：1.637

闪光点：239.8°C

储存条件：Desiccate at +4°C

PSA：51.80000

LOGP：5.52470

参考文献

[1]. Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82.

[2]. Bassil AK, et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. Br J Pharmacol. 2009 Sep;158(1):252-8