AZD1981

Catalog No.S7263

AZD1981 Chemical Structure

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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Biological Activity

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.
Targets
CRTh2 (DP2) receptor [1]
4 nM
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]

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]

Protocol

Solubility (25°C)

In vitro DMSO 11 mg/mL (28.28 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.87
Formula

C19H17ClN2O3S

CAS No. 802904-66-1
Storage powder
in solvent
Synonyms N/A

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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

Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID