AZD1981 | 99.82%(HPLC) | In Stock

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: 802904-66-1

Selleck's AZD1981 has been cited by 1 publication

Purity & Quality Control

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

99.82

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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
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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Luker T, et al. Bioorg Med Chem Lett. 2011, 21(21), 6288-6292. [2] Schmidt JA, et al. Br J Pharmacol. 2013, 168(7), 1626-1638.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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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