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BI-671800 (Synonyms: AP-761)

Catalog No.GC31757

An antagonist of CRTH2/DP2

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BI-671800 Chemical Structure

Cas No.: 1093108-50-9

Size Price Stock Qty
10mM (in 1mL DMSO)
$284.00
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5mg
$258.00
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10mg
$441.00
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25mg
$873.00
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50mg
$1,517.00
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100mg
$2,436.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

BI-671800 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[1]. BI-671800 has potential for the treatment of poorly controlled asthma[2].

BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells[1].

BI-671800 (compound A, 0.1-10 mg/kg, i.g.) shows significant inhibition of AHR in mice[1]. BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals[3].|| Animal Model:|6-8-week-old age- and sex-matched BALB/c mice (mice were sensitized for 14 days, challenged intranasally)[1].|Dosage:|10-0.1 mg/kg|Administration:|Oral gavage for 4 weeks|Result:|Shows significant inhibition of AHR in mice.

[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.

Chemical Properties

Cas No. 1093108-50-9 SDF
Synonyms AP-761
Canonical SMILES O=C(O)CC1=C(N(C)C)N=C(CC2=CC=C(NC(C3=CC=C(C(F)(F)F)C=C3)=O)C=C2)N=C1N(C)C
Formula C25H26F3N5O3 M.Wt 501.5
Solubility DMSO : 135 mg/mL (269.19 mM) Storage 4°C, protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.994 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.994 mL 3.988 mL
10 mM 0.1994 mL 0.997 mL 1.994 mL
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 33 reference(s) in Google Scholar.)

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