產(chǎn)品屬性:
產(chǎn)品名稱 | WOBE437 |
規(guī)格 | 1mg、5mg、10mg |
貨號 | EY-01Y17394 |
Cas No.: 2108100-73-6
別名: N/A
化學(xué)名: N/A
分子式: C22H33NO3
分子量: 359.5
溶解度: DMF: 2.5 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 1 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
WOBE437 is a potent endocannabinoid uptake inhibitor with IC50 values of 10 and 283 nM for arachidonoyl ethanolamide and 2-arachidonoyl glycerol uptake, respectively, in U937 cells. It is greater than 1,000-fold selective for endocannabinoid transporters over fatty acid amide hydrolase and the 2-AG hydrolyzing enzymes MAGL, ABHD6, and ABHD12. WOBE437 inhibits AEA uptake in FAAH-deficient HMC-1 human mast cells and Neuro2a mouse neuroblastoma cells (IC50s = 137 and 55 nM, respectively) and reduces AEA uptake by 50% in rat cortical neurons when used at a concentration of 1 μM. It also reduces 2-AG uptake by 40% in Neuro2a cells at a concentration of 5 μM. In vivo, WOBE437 increases AEA and 2-AG levels by 1.5-fold in mouse brain but not peripheral tissues after intraperitoneal administration of a 10 mg/kg dose for seven days. WOBE437 (10 mg/kg) also induces a typical tetrad of hypothermia, catalepsy, analgesia, and hypomotility in mice, indicating it also acts as an indirect cannabinoid (CB) receptor 1 agonist.
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