Molecular Weight(MW): 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.
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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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Molecular Weight Calculator
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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