DO34-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDO34Cat. No.: HY-117771CAS No.: 1848233-58-8分式: CHFNO分量: 531.53作靶点: Others作通路: Others储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (188.14 mM)* means soluble, but saturation unk

2、nown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8814 mL 9.4068 mL 18.8136 mL5 mM 0.3763 mL 1.8814 mL 3.7627 mL10 mM 0.1881 mL 0.9407 mL 1.8814 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以

3、下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (18.81 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (18.81 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www

4、.MedChemESolubility: 10 mg/mL (18.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DO34个强效的、选择性的酰 油脂肪酶 (DAGL) 的中性活性抑制剂，其对 DAGL 转换的 IC50 值为6 nM，对 DAGL 的IC50 值为 3-8 nM。IC50 & Target IC50: 6 nM (DAGL), 3-8 nM (DAGL) 1.体外研究 DO34 is a highly potent, selective and centrally active DAGL inhibitor, with an IC50

5、 of 6 nM for DAGLconversion of SAG to 2-AG, as determined using a real-time, fluorescence-based natural substrate assaywith membrane lysates from HEK293T cells expressing recombinant human DAGL. It is also confirmed thatand DO34 is a potent inhibitor of DAGL with IC50 of 3-8 nM 1.体内研究 DO34 (compound

6、 39) prevents fasting-induced refeeding of mice, which is typical cannabinoid CB1-receptormediated behavior. DO34 (comound 39) reduces brain 2-AG levels in dose- and time dependent manner 2.DO34 could block the tonic CB1 activation. AM251 significantly increases basal PF-EPSCs in MAGL-TKOmice, and t

7、he effect of AM251 is blocked by the DAGL inhibitor DO34 3.PROTOCOLAnimal Mice 2Administration 2 12-week-old male C57Bl/6J mice are single housed in metabolic cages with a regular 12:12h light/dark cycle(6 a.m.-6 p.m.) and free access to food and water unless noted otherwise. After 3 days of acclima

8、tization,mice are fasted for 18h starting at midnight followed by an intraperitoneal injection with 38 (50 mg/kg), DO34(compound 39: 50 mg/kg), 40 (50 mg/kg) or vehicle 30 min prior to refeeding 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENC

9、ES1. Ogasawara D, et al. Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition. Proc NatlAcad Sci U S A. 2016 Jan 5;113(1):26-33.2. Deng H, et al. Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. J Med Chem. 2017 Jan12;60(1):428-440.3. Liu X, et al. Coordinated regulation of endocannabinoid-mediated retrograde synaptic suppression in the cerebellum by neuronal andastrocytic monoacylglycerol lipase. Sci Rep. 2016 Oct 24;6:35829.McePdfHeightCaution: Product has not been fully validate