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BI-671800 (AP-761) 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. BI-671800 has the potential to treat poorly controlled asthma[2].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $44 | In Stock | In Stock | |
| 5 mg | $108 | In Stock | In Stock | |
| 10 mg | $179 | In Stock | In Stock | |
| 25 mg | $326 | In Stock | In Stock | |
| 50 mg | $463 | In Stock | In Stock | |
| 100 mg | $629 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $122 | In Stock | In Stock |
| Description | BI-671800 (AP-761) 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. BI-671800 has the potential to treat poorly controlled asthma[2]. |
| Targets&IC50 | CRTH2 (mouse):3.7 nM (in CRTH2 transfected cells), CRTH2 (human):4.5 nM (in CRTH2 transfected cells) |
| In vitro | BI-671800 (compound A) is a potent small-molecule antagonist with low nanomolar potency against human or mouse CRTH2 in transfected cells[1]. |
| In vivo | BI-671800 (compound A, 0.1-10 mg/kg, i.g.) significantly inhibits AHR in mice[1] and effectively prevents edema formation, reduces inflammatory infiltrate, and alleviates skin pathology observed in drug vehicle-treated animals[3]. |
| Synonyms | Cmpd A, AP-761 |
| Molecular Weight | 501.5 |
| Formula | C25H26F3N5O3 |
| Cas No. | 1093108-50-9 |
| Smiles | CN(C)c1nc(Cc2ccc(NC(=O)c3ccc(cc3)C(F)(F)F)cc2)nc(N(C)C)c1CC(O)=O |
| Relative Density. | 1.351 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 130 mg/mL (259.22 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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