BI-671800

For research use only.

Catalog No.S0495 Synonyms: AP-761, Cmpd A

BI-671800 Chemical Structure

CAS No. 1093108-50-9

BI-671800 (AP-761, Cmpd A) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to human CRTH2 and murine CRTH2, respectively. BI-671800 is associated with a small improvement in FEV1 in symptomatic controller-naïve asthma patients, and in patients on ICS.

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Biological Activity

Description BI-671800 (AP-761, Cmpd A) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to human CRTH2 and murine CRTH2, respectively. BI-671800 is associated with a small improvement in FEV1 in symptomatic controller-naïve asthma patients, and in patients on ICS.
Targets
murine CRTH2 [1]
(Cell-free assay)
human CRTH2 [1]
(Cell-free assay)
3.7 nM 4.5 nM

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (199.4 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 501.50
Formula

C25H26F3N5O3

CAS No. 1093108-50-9
Storage powder
in solvent
Synonyms AP-761, Cmpd A
Smiles CN(C)C1=C(C(=NC(=N1)CC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)C(F)(F)F)N(C)C)CC(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01216384 Completed Drug: BI 671800|Drug: placebo Asthma|Rhinitis Allergic Perennial Boehringer Ingelheim October 2010 Phase 1
NCT01215773 Completed Drug: Placebo|Drug: BI 671800 Healthy Boehringer Ingelheim October 2010 Phase 1
NCT01205373 Completed Drug: BI 671800 Healthy Boehringer Ingelheim September 2010 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID