化合物ARN19702 T9528

Product Introduction
Bioactivity


英文名: ARN19702

描述: ARN19702 是一种选择性，具有口服活性的，可逆的，可透过血脑屏障的 N-乙酰乙醇胺酸酰胺酶 (NAAA) 抑制剂，对人 NAAA 的 IC50为 230 nM。ARN19702 具有广泛的镇痛作用。

体内活性: ARN19702 (3-10 mg/kg; po; daily; for 7 consecutive days) reduces nociception associated with Paclitaxel-induced neuropathy without development of subacute antinociceptive tolerance in male rats [1]. In male mice, ARN19702 (0.1-30 mg/kg; po) dose-dependently reduces the spontaneous nocifensive response elicited by intraplantar formalin injection and the hypersensitivity caused by intraplantar carrageenan injection, paw incision, or sciatic nerve ligation [1].. ARN19702 (3-10 mg/kg; po) produces remarkable protective effects against multiple sclerosis in mice [2]. Pharmacokinetic properties of ARN19702 in mice 3 mg/kg,i.v 3 mg/kg, p.o. C max (ng/mL) 1660±166 613±68 T max (min) (5.0) 30 CL (mL/min/Kg) 33.2±1.6 49±8 t 1/2 (min) 73.9±3.7 104±16 AUC plasma (h×ng/mL) 1366.8±68.3 988±157 AUC brain (h×ng/mL) 404.3±109.1 181±28 F (%) - 72±11

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

溶解度: DMSO : 50 mg/mL (111.72 mM)


关键字: ARN19702 | ARN 19702 | ARN-19702

相关库: Bioactive Compounds Library Max | Inhibitor Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途