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AZD1981 802904-66-1

Product Description

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Molecular Weight:

388.87 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.

Biological Activity

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 [3H]PGD2 to mouse, rat, guinea pig, rabbit and dog recombinant DP2.


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.

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Product Categories : Endocrinology & Hormones > GPR Inhibitor