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AZD1981

Catalog No. T6399 CAS 802904-66-1

Synonyms: Prostaglandin Receptor, AZD 1981, AZD1981, Inhibitor, AZD-1981, inhibit

AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of Asthma, Postmenopausal, Pharmakokinetic, Asthma Patients, and Drug Interaction, among others.

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AZD1981, CAS 802904-66-1

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD1981 is an effective and specific CRTh2 (DP2) receptor antagonist (IC50: 4 nM), showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. AZD1981 has been used in trials studying the treatment and basic science of Asthma, Postmenopausal, Pharmakokinetic, Asthma Patients, and Drug Interaction, among others.
Targets&IC50	CRTh2 (DP2) receptor: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]

Synonyms	Prostaglandin Receptor, AZD 1981, AZD1981, Inhibitor, AZD-1981, inhibit
Molecular Weight	388.87
Formula	C19H17ClN2O3S
CAS No.	802904-66-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

H2O: <1 mg/mL

DMSO: 9 mg/mL (23.1 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library GPCR Compound Library Endocrinology-Hormone Compound Library Inhibitor Library Immunology/Inflammation Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.