RS-127445 hydrochloride

Chemical Structure : RS-127445 hydrochloride

CAS No.: 199864-86-3

加入收藏

货号: PC-27111Not For Human Use, Lab Use Only.

规格	价格	库存
25 mg	￥780	In stock
50 mg	￥1180	In stock
100 mg	￥1980	In stock
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

RS-127445 hydrochloride is a potent, selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with pKi of 9.5, 1,000 fold selectivity over numerous other receptor and ion channel binding sites.
RS-127445 potently antagonizes 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) in cells expressing human recombinant 5-HT2B receptors.
RS-127445 also blocks 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).
RS-127445 (5 mg/kg, i.p.) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h.

物理化学性质&存储条件

分子量	317.79
分子式	C17H17ClFN3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine hydrochloride

参考文献

1. Kelly CR, et al. J Pharmacol Exp Ther. 2006 Jun;317(3):1254-61.

2. Bonhaus DW, et al. Br J Pharmacol. 1999 Jul;127(5):1075-82.