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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 | Availability | Quantity |
---|---|---|---|
1 mg | $53 | In Stock | |
5 mg | $133 | In Stock | |
10 mg | $218 | In Stock | |
25 mg | $392 | In Stock | |
50 mg | $557 | In Stock | |
100 mg | $756 | In Stock | |
200 mg | $987 | In Stock | |
1 mL x 10 mM (in DMSO) | $147 | 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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 130 mg/mL (259.22 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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