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BI 671800

  Cat. No.:  DC20781   Featured
Chemical Structure
1093108-50-9
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More than 5000 active chemicals with high quality for research!
Field of application
BI 671800 is a potent, oral prostaglandin D2 receptor (CRTH2) antagonist for treatment of asthma..
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1093108-50-9
Chemical Name: 4,6-bis(dimethylamino)-2-((4-((4-(trifluoromethyl)benzoyl)amino)phenyl)methyl)-5-pyrimidineacetic acid
Synonyms: BI671800,AP-761,AP761,AP 761
SMILES: CN(C)C1=NC(CC2=CC=C(NC(C3=CC=C(C(F)(F)F)C=C3)=O)C=C2)=NC(N(C)C)=C1CC(O)=O
Formula: C25H26F3N5O3
M.Wt: 501.5
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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].
Target: hCRTH2:4.5 nM (IC50, in CRTH2 transfected cells) mCRTH2:3.7 nM (IC50, in CRTH2 transfected cells)
In Vivo: 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].
In Vitro: BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells[1].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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