For research use only.
CAS No. 802904-66-1
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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|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.|
|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 [3H]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. |
|In vitro||DMSO||11 mg/mL (28.28 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02367066||Completed||Drug: AR-C165395XX|Other: Placebo||Type 2 Diabetes Mellitus||AstraZeneca||March 2015||Phase 1|
|NCT02031679||Completed||Drug: AZD1981|Drug: Placebo||Chronic Idiopathic Urticaria||Johns Hopkins University|AstraZeneca||January 2014||Phase 2|
|NCT01199341||Completed||Drug: AZD1981|Drug: Warfarin||Pharmakokinetic||AstraZeneca||October 2010||Phase 1|
|NCT01196689||Completed||Drug: AZD1981 100 mg twice daily for 61/2 days||Asthma||AstraZeneca||October 2010||Phase 1|
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