化合物GW842166X T6527

Product Introduction
Bioactivity


英文名: GW842166X

描述: GW842166X 是一种选择性 cannabinoid receptor 2 激活剂，IC50=63 nM。

体外活性: GW842166X shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63 nM, respectively. [1] GW-842166X exhibits full agonist potency with an EC50 of 133 nM and Emax of 101% in cyclase assays. GW-842166X exhibits weak agonist potency with an EC50 of 7.780 μM and Emax of 84% in FLIPR assays. [2]

体内活性: GW842166X has an oral bioavailability of 58% and a half-life of 3 h when dosed orally in the rat. GW842166X has extremely high potency with an oral ED50 of 0.1 mg/kg and shows full reversal of hyperalgesia at 0.3 mg/kg in the FCAa model of inflammatory pain. [1] GW842166X orally administrated at a dose of 15 mg/kg for 8 days produced a significant reversal of the CCI induced decrease in paw withdrawal threshold in a rat model of neuropathic pain. [3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 16 mg/mL (35.6 mM)


关键字: inhibit | Cannabinoid Receptor | GW-842166X | Inhibitor | GW842166X

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Covalent Inhibitor Library | Anti-Alzheimer's Disease Compound Library

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