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BI-671800

Catalog No. T14565   CAS 1093108-50-9
Synonyms: AP-761, Cmpd A

BI-671800 (AP-761) 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 Chemical Structure
BI-671800, CAS 1093108-50-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 92.00
2 mg In stock $ 135.00
5 mg In stock $ 228.00
10 mg In stock $ 397.00
25 mg In stock $ 663.00
50 mg In stock $ 945.00
100 mg In stock $ 1,280.00
500 mg In stock $ 2,570.00
1 mL * 10 mM (in DMSO) In stock $ 253.00
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Purity: 98.06%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BI-671800 (AP-761) 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 mCRTH2:3.7 nM (in CRTH2 transfected cells), hCRTH2:4.5 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 AP-761, Cmpd A
Molecular Weight 501.5
Formula C25H26F3N5O3
CAS No. 1093108-50-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 130 mg/mL (259.22 mM), sonification is recommended.

TargetMolReferences 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Inhibitor Library ReFRAME Related Library Bioactive Compounds Library Max GPCR Compound Library Bioactive Compound Library NO PAINS Compound Library Endocrinology-Hormone Compound Library Immunology/Inflammation Compound Library

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Keywords

BI-671800 1093108-50-9 Endocrinology/Hormones GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor GPR BI 671800 Inhibitor AP 761 inhibit BI671800 AP-761 AP761 Cmpd A inhibitor

 

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