 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 802904-66-1 |
| Molecular formula(MF) | C19H17ClN2O3S |
| Molecular Weight(MW): | 388.87 |
| Alias |
| In vitro | DMSO | 11 mg/mL (28.28 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL |
| Description | AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. | ||
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| Features | An orally available selective DP2(CRTh2) receptor antagonist in clinical development for asthma. | ||
| Targets |
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| In vitro |
AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM. [1] AZD1981 blocks DP2-mediated shape change in human eosinophils and basophils in blood, as well as DP2-mediated chemotaxis of human Th2 cells and eosinophils. Moreover, AZD1981 also blocks the binding of [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2. [2] |
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| In vivo | AZD1981 has high oral bioavailability in male sprague dawley rats. [1] In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization. [2] |