Home GPCR & G Protein Prostaglandin Receptor antagonist BI-671800 For research use only.

BI-671800

Synonyms: AP-761, Cmpd A

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.

BI-671800 Chemical Structure

BI-671800 Chemical Structure

CAS: 1093108-50-9

Purity & Quality Control

Batch: S049501 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.34%
99.34

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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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01216384 Completed
Asthma|Rhinitis Allergic Perennial
Boehringer Ingelheim
 October 2010 Phase 1
NCT01215773 Completed
Healthy
Boehringer Ingelheim
 October 2010 Phase 1
NCT01205373 Completed
Healthy
Boehringer Ingelheim
 September 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 501.50 Formula

C25H26F3N5O3
CAS No. 1093108-50-9 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (199.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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