Home Endocrinology & Hormones GPR antagonist AZD1981 For research use only.

AZD1981

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

AZD1981 Chemical Structure

CAS No. 802904-66-1

Purity & Quality Control

Batch: S726301 DMSO]11 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.82%
99.82

AZD1981 Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02367066 Completed
Type 2 Diabetes Mellitus
AstraZeneca
 March 2015 Phase 1
NCT02031679 Completed
Chronic Idiopathic Urticaria
Johns Hopkins University|AstraZeneca
 January 2014 Phase 2
NCT01199341 Completed
Pharmakokinetic
AstraZeneca
 October 2010 Phase 1
NCT01196689 Completed
Asthma
AstraZeneca
 October 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 388.87 Formula

C19H17ClN2O3S
CAS No. 802904-66-1 SDF Download AZD1981 SDF
Smiles CC1=C(C2=C(C=CC=C2N1CC(=O)O)NC(=O)C)SC3=CC=C(C=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 11 mg/mL ( (28.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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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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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