Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
AZD1981 is a potent, selective antagonist with of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2.
Features
An orally available selective DP2(CRTh2) receptor antagonist in clinical development for asthma.
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. 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 [H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2.
In vivo
AZD1981 has high oral bioavailability in male sprague dawley rats. In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization.
