Home GPCR & G Protein Prostaglandin Receptor antagonist BI-671800

research use only

BI-671800 Prostaglandin Receptor antagonist

Cat.No.S0495

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. This compound is associated with a small improvement in FEV1 in symptomatic controller-naïve asthma patients, and in patients on ICS.
BI-671800 Prostaglandin Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 501.50

Jump to

Quality Control

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 501.50 Formula

C25H26F3N5O3

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

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

Mechanism of Action

Targets/IC50/Ki
murine CRTH2
(Cell-free assay)
3.7 nM
human CRTH2
(Cell-free assay)
4.5 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.