AZD1981

Catalog No.S7263

For research use only.

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.

AZD1981 Chemical Structure

CAS No. 802904-66-1

Selleck's AZD1981 has been cited by 1 Publication

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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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 388.87
Formula

C19H17ClN2O3S

CAS No. 802904-66-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C2=C(C=CC=C2N1CC(=O)O)NC(=O)C)SC3=CC=C(C=C3)Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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