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。
产品描述
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC 50 of 230 nM for human NAAA. ARN19702 exhibits a broad analgesic profile [1] [2].
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
Cas No.
1971937-18-4
分子式
C21H22FN3O3S2
分子量
447.54
别名
ARN19702
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years