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BI-671800

Cat. No. M20981
BI-671800 Structure
Synonym:

AP-761, Cmpd A

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Biological Activity

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.

Chemical Information
Molecular Weight 501.5
Formula C25H26F3N5O3
CAS Number 1093108-50-9
Solubility (25°C) DMSO 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David Miller, et al. Allergy Asthma Proc. A randomized study of BI 671800, a CRTH2 antagonist, as add-on therapy in poorly controlled asthma

[2] Ibrahim Sulaiman, et al. Pulm Pharmacol Ther. Molecularly targeted therapies for asthma: Current development, challenges and potential clinical translation

[3] Ian P Hall, et al. Pulm Pharmacol Ther. Efficacy of BI 671800, an oral CRTH2 antagonist, in poorly controlled asthma as sole controller and in the presence of inhaled corticosteroid treatment

[4] Norbert Krug, et al. J Allergy Clin Immunol. Efficacy of the oral chemoattractant receptor homologous molecule on TH2 cells antagonist BI 671800 in patients with seasonal allergic rhinitis

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Keywords: BI-671800, AP-761, Cmpd A supplier, Prostaglandin Receptor, inhibitors, activators
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