GW842166X

SKU: orb1221905

Description

GW 842166X is a cannabinoid receptor 2 (CB2) agonist potentially for the treatment of inflammatory pain.(In Vitro):GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors. It has no significant agonist activity at concentrations up to 30 μM in human and rat CB1 recombinant assays.(In Vivo):GW842166X has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and shows full reversal of hyperalgesia at 0.3 mg/kg. The blood concentrations of GW842166X in experiments are 30 nM (0.03 mg/kg), 130 nM (0.1 mg/kg), and 370 nM (0.3 mg/ kg) 1 h after dosing. After dosing for 4 days in the FCA model, no statistical difference in antihyperalgesic response is observed on day 4 relative to day 1, indicating that tolerance does not occur.

Key Properties

• CAS Number: 666260-75-9
• MW: 449.25
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₇Cl₂F₃N₄O₂
• SMILES: FC(F)(F)C1=NC(NC2=CC=C(Cl)C=C2Cl)=NC=C1C(=O)NCC1CCOCC1
• Target: Topoisomerase
• Solubility: DMSO : ≥ 83.3 mg/mL; 185.42 mM

Bioactivity

• In Vivo:
  GW842166X has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and shows full reversal of hyperalgesia at 0.3 mg/kg. The blood concentrations of GW842166X in experiments are 30 nM (0.03 mg/kg), 130 nM (0.1 mg/kg), and 370 nM (0.3 mg/ kg) 1 h after dosing. After dosing for 4 days in the FCA model, no statistical difference in antihyperalgesic response is observed on day 4 relative to day 1, indicating that tolerance does not occur.
• In Vitro:
  GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors. It has no significant agonist activity at concentrations up to 30 μM in human and rat CB1 recombinant assays.

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

GW-842166X | 842166X | 842166

Quick Database Links

Gene Symbol

Topoisomerase