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CRTH2-IN-1
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图片
CAS NO:926661-54-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
Ramatroban analog
产品介绍
CRTH2-IN-1 (Ramatroban analog) 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 6 nM。
生物活性

CRTH2-IN-1 (Ramatroban analog) is a selectiveprostaglandin D2 receptor DP2(CRTH2) antagonist with an IC50of 6 nM in a human DP2 binding assay.

IC50& Target

CYP3A4

7 μM (IC50)

CYP 2C9

5 μM (IC50)

体外研究
(In Vitro)

CRTH2-IN-1 (Ramatroban analog, Compound 5) is a novel prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50of 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 using3H-PGD2 and human platelet membranes. Human thromboxane receptor (hTP) binding performed using human platelet membranes and3H-SQ-29,548. Human prostacyclin receptor (hIP) binding perfomed using hIP/293 membranes and3Hiloprost. CRTH2-IN-1 inhibits hDP1 binding with an IC50of 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].

分子量

416.47

Formula

C21H21FN2O4S

CAS 号

926661-54-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.