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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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