AZD1981

SKU: orb1300801

Description

AZD1981 is a potent and selective CRTh2 (DP2) receptor antagonist with an IC50 of 4 nM, demonstrating over 1000-fold selectivity against DP1 and numerous other targets. It has been utilized in both in vitro mechanistic studies and in vivo clinical trials investigating asthma and other inflammatory conditions.

Research Area

Immunology & Inflammation, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 802904-66-1
• MW: 388.87
• Purity: 99.54%
• Formula: C₁₉H₁₇ClN₂O₃S
• SMILES: CC(=O)Nc1cccc2n(CC(O)=O)c(C)c(Sc3ccc(Cl)cc3)c12
• Target: Prostaglandin Receptor,GPCR
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+90% Corn Oil:0.5 mg/mL (1.29 mM);DMSO:9 mg/mL (23.14 mM)

Bioactivity

• Target IC50:
  CRTh2 (DP2) receptor:4 nM
• In Vivo:
  AZD1981 has high oral bioavailability in male sprague dawley rats. In guinea pig hind limb model, AZD1981 (100 nM) completely inhibits DK-PGD2-induced eosinophil mobilization.
• 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. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ProstaglandinReceptor, Prostaglandin Receptor, AZD 1981, AZD1981, AZD-1981, CRTh2 (DP2) receptor, Inhibitor, inhibit

Compound Identifiers

PubChem CID

11292191