BI-671800

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].

Product Specifications

CAS Number

[1093108-50-9]

Product Name Alternative

Cyclopamine-KAAD

UNSPSC

12352005

Target

CRTH2 (GPR44) ; Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/BI-671800.html

Concentration

10mM

Purity

99.36

Solubility

DMSO : 135 mg/mL (ultrasonic)

Smiles

O=C(O)CC1=C(N(C)C)N=C(CC2=CC=C(NC(C3=CC=C(C(F)(F)F)C=C3)=O)C=C2)N=C1N(C)C

Molecular Formula

C25H26F3N5O3

Molecular Weight

501.50

References & Citations

[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.