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BI-671800
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。
BI-671800图片
CAS NO:1093108-50-9
规格:98%
分子量:501.5
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
BI-671800是高特异性的、有效的前列腺素D2受体(DP2/CRTH2)的拮抗剂,其对人和小鼠CRTH2转染细胞中PGD2结合CRTH2的IC50值分别为4.5nM和3.7nM。有治疗哮喘的潜能。
CAS:1093108-50-9
分子式:C25H26F3N5O3
分子量:501.5
纯度:98%
存储:Store at -20°C

Background:

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2), with IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively[1]. BI-671800 has potential for the treatment of poorly controlled asthma[2].


BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells[1].


BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice[1]. BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3].|| Animal Model:|6-8-week-old age- and sex-matched BALB/c mice (mice were sensitized for 14 days, challenged intranasally)[1].|Dosage:|10-0.1 mg/kg|Administration:|Oral gavage for 4 weeks|Result:|Shows significant inhibition of AHR in mice.


[1]. Boehme SA, et al. A small molecule CRTH2 antagonist inhibits FITC-induced allergic cutaneous inflammation. Int Immunol. 2009 Jan;21(1):81-93. [2]. Miller D, et al. A randomized study of BI 671800, a CRTH2 antagonist, as add-on therapy in poorly controlled asthma. Allergy Asthma Proc. 2017 Mar 1;38(2):157-164. [3]. Lukacs NW, et al. CRTH2 antagonism significantly ameliorates airway hyperreactivity and downregulates inflammation-induced genes in a mouse model of airway inflammation. Am J Physiol Lung Cell Mol Physiol. 2008 Nov;295(5):L767-79.