CAS NO: | 1971937-18-4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cas No. | 1971937-18-4 |
分子式 | C21H22FN3O3S2 |
分子量 | 447.55 |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects[1][2]. 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) attenuates in a dose-dependent manner 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. Cmax (ng/mL)1660±166613±68 Tmax (min)(5.0)30 CL (mL/min/Kg)33.2±1.649±8 t1/2 (min)73.9±3.7104±16 AUCplasma (h×ng/mL)1366.8±68.3988±157 AUCbrain (h×ng/mL)404.3±109.1181±28 F (%)-72±11 [1]. Yannick Fotio, et al. Antinociceptive Profile of ARN19702, (2-Ethylsulfonylphenyl)-[(2S)-4-(6-fluoro-1,3-benzothiazol-2-yl)-2-methylpiperazin-1-yl]methanone, a Novel Orally Active N-Acylethanolamine Acid Amidase Inhibitor, in Animal Models. J Pharmacol Exp Ther. 2021 Aug;378(2):70-76. |