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BI-671800

Catalog No. T14565   CAS 1093108-50-9
Synonyms: BI-671800, BI671800, Inhibitor, BI 671800, Prostaglandin Receptor, Cmpd A, inhibit, AP-761

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. BI-671800 has the potential to treat poorly controlled asthma[2].

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BI-671800, CAS 1093108-50-9
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
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. BI-671800 has the potential to treat poorly controlled asthma[2].
Targets&IC50 hCRTH2:4.5 nM (in CRTH2 transfected cells), mCRTH2:3.7 nM (in CRTH2 transfected cells)
In vitro BI-671800 (compound A) exhibits low nM potency as a potent small-molecule antagonist of human or mouse CRTH2 in transfected cells[1].
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) also effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3].
Synonyms BI-671800, BI671800, Inhibitor, BI 671800, Prostaglandin Receptor, Cmpd A, inhibit, AP-761
Molecular Weight 501.5
Formula C25H26F3N5O3
CAS No. 1093108-50-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 130 mg/mL (259.22 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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.

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