AZD 2098

SKU: orb1224644

Description

AZD2098 is a potent, selective, orally bioavailable CCR4 receptor antagonist with pIC50 of 7.8 for hCCR4, pIC50 of 8.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.3; exhibits anti-inflammatory effects in Brown-Norway rats sensitized to ovalbumin.Asthma Phase 1 Clinical.

Key Properties

• CAS Number: 566203-88-1
• MW: 334.171
• Purity: >98% (HPLC)
• Formula: C₁₁H₉Cl₂N₃O₃S
• SMILES: O=S(C1=CC=CC(Cl)=C1Cl)(NC2=NC=CN=C2OC)=O
• Target: Chemokine Receptor
• Solubility: DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  AZD2098 (73.5-5.0 μg/kg; p.o. ; BID; twice a day; 1 hour before and every 12 hours after antigen challenge) exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats, and the changes are first visible at a dose of 0.22 μmol/kg and maximal at 7.5 μmol/kg. Animal model: Brown-Norway rats. Dosage: 73.5 μg/kg, 250.6 μg/kg, 735.2 μg/kg, 1.0 mg/kg, 2.5 mg/kg, 5.0 mg/kg. Administration: Oral administration; twice a day; 1 hour before and every 12 hours after antigen challenge. Result: Exhibits efficacy against antigen-induced inflammatory response among ovalbumin-sensitized rats.
• In Vitro:
  AZD2098 potently inhibits chemokine-induced cellular responses, with pIC50 of 7.5 and 6.3 against CCL22-induced Ca2+ influx in hCCR4-expressing CHO cells and CCL17- or CCL22-induced chemotaxis of primary human Th2 cells respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD2098 | AZD-2098

Quick Database Links

Gene Symbol

Chemokine Receptor