GW842166X

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GW842166X 是一种有效且高度选择性的大麻素受体 CB2 受体激动剂，EC50 为 63 nM，对 CB1 受体没有显着活性。

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.

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.

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.

GW-842166X | 842166X | 842166

Cell Cycle/DNA Damage

Topoisomerase

CB2

Others-Field

——

666260-75-9

449.25

C18H17Cl2F3N4O2

>98% (HPLC)

DMSO : ≥ 83.3 mg/mL; 185.42 mM

FC(F)(F)C1=NC(NC2=CC=C(Cl)C=C2Cl)=NC=C1C(=O)NCC1CCOCC1

2-((2,4-dichlorophenyl)amino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years