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CRTH2-IN-1(Ramatroban analog)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CRTH2-IN-1(Ramatroban analog)图片
CAS NO:926661-54-3
规格:98%
分子量:416.47
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
CRTH2-IN-1(Ramatrobananalog)是一种选择性的前列腺素D2受体DP2(CRTH2)拮抗剂,在人类DP2结合试验中IC50为6nM。
CAS:926661-54-3
分子式:C21H21FN2O4S
分子量:416.47
纯度:98%
存储:Store at -20°C

Background:

CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.


CRTH2-IN-1 (Ramatroban analog, Compound 5) is a novel prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 7 nM in a human whole blood eosinophil shape change assay (hESC). CRTH2-IN-1 (Ramatroban analog) is a novel tricyclic antagonist of the prostaglandin D2 receptor DP2 (CRTH2) with efficacy in a murine model of allergic rhinitis. Human prostaglandin D1 receptor (hDP1) binding is performed using 3H-PGD2 and human platelet membranes. Human thromboxane receptor (hTP) binding performed using human platelet membranes and 3H-SQ-29,548. Human prostacyclin receptor (hIP) binding perfomed using hIP/293 membranes and 3Hiloprost. CRTH2-IN-1 inhibits hDP1 binding with an IC50 of 1μM. CRTH2-IN-1 inhibits hTP and hIP binding with IC50s of >100 μM. CRTH2-IN-1 inhibits human CYP isoforms CYP3A4, CYP 2C9 and CYP2D6 with IC50s of 7, 5 and >30 μM, respectively[1].



[1]. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51.