DO34-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDO34Cat. No.: HY-117771CAS No.: 1848233-58-8分式: CHFNO分量: 531.53作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (188.14 mM)* means soluble, but saturation unk

2、nown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以

3、下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 10 mg/mL (18.81 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 10 mg/mL (18.81 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www

4、.MedChemESolubility: 10 mg/mL (18.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DO34個(gè)強(qiáng)效的、選擇性的酰 油脂肪酶 (DAGL) 的中性活性抑制劑，其對(duì) DAGL 轉(zhuǎn)換的 IC50 值為6 nM，對(duì) DAGL 的IC50 值為 3-8 nM。IC50 & Target IC50: 6 nM (DAGL), 3-8 nM (DAGL) 1.體外研究 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.體內(nèi)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