Potent soluble epoxide hydrolase (sEH) inhibitor (IC50 values are 1.1 and 2.1 nM for murine and human receptor, respectively). Inhibits MAPK and NF-κB signaling, as well as reducing ER stress and cell death in models of pancreatitis. Exhibits antidepressant effects in a social defeat stress model. Orally bioavailable and brain penetrant.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Sumanta Kumar Goswami,et al. Anti-Ulcer Efficacy of Soluble Epoxide Hydrolase Inhibitor TPPU on Diclofenac-Induced Intestinal Ulcers. J Pharmacol Exp Ther. 2016 Jun; 357(3): 529–536. Published online 2016 Jun. doi: 10.1124/jpet.116.232108.
[2] Arzu Ulu,et al. An Omega-3 Epoxide of Docosahexaenoic Acid Lowers Blood Pressure in Angiotensin-II Dependent Hypertension. J Cardiovasc Pharmacol. Author manuscript; available in PMC 2015 Jul 1.Published in final edited form as: J Cardiovasc Pharmacol. 2014 Jul; 64(1): 87–99. doi: 10.1097/FJC.0000000000000094.
分子式 C16H20F3N3O3 |
分子量 359.34 |
CAS号 1222780-33-7 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water <1 mg/mL |
Ethanol 50 mM |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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