ARN19702

ARN19702CAS号: 1971937-18-4分子式: C21H22FN3O3S2分子量: 447.55描述纯度储存/保存方法可溶性/溶解性靶点In vivo(体内研究)

产品描述
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].
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:50 mg/mL (111.72 mM)
生物活性
靶点
N-acylethanolamine acid amidase (NAAA):230 nM
In vivo(体内研究)
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