LY2183240 - FAAH 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELY2183240Cat. No.: HY-10865CAS No.: 874902-19-9分式: CHNO分量: 307.35作靶点: FAAH作通路: Metabolic Enzyme/Protease; Neuronal Signaling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 : 50 mg/mL (162.68

2、mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.2536 mL 16.2681 mL 32.5362 mL5 mM 0.6507 mL 3.2536 mL 6.5072 mL10 mM 0.3254 mL 1.6268 mL 3.2536 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

3、备液可以根据储存条件，适当保存；以下溶剂前的百分 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 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.13 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.13 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 LY21832

4、40活性素吸收阻断剂，IC50为270 pM，还能抑制脂 酸酰胺解酶（FAAH），IC50为12.4nM。户使本产品发表的科研献 Eur J Pain. 2017 May;21(5):804-814.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Dickason-Chesterfield AK, et al. Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolaseinhib

5、itors. Cell Mol Neurobiol. 2006 Jul-Aug;26(4-6):407-23.2. Alexander JP, Cravatt BF. The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several otherbrain serine hydrolases. J Am Chem Soc. 2006 Aug 2;128(30):9699-704.3. Maione S, et al. Antinociceptive effects

6、of tetrazole inhibitors of endocannabinoid inactivation: cannabinoid and non-cannabinoidreceptor-mediated mechanisms. Br J Pharmacol. 2008 Nov;155(5):775-82.4. Pelorosso FG, et al. The endocannabinoid anandamide inhibits kinin B1 receptor sensitization through cannabinoid CB1 receptorstimulation in

7、human umbilical vein. Eur J Pharmacol. 2009 Jan 5;602(1):176-9.5. Powers MS, et al. Effects of the novel endocannabinoid uptake inhibitor, LY2183240, on fear-potentiated startle and alcohol-seekingbehaviors in mice selectively bred for high alcohol preference. Psychopharmacology (Berl). 2010 Dec;212(4):571-83.6. Sun L, et al. Endocannabinoid activation of CB1 receptors contributes to long-lasting reversal of neuropathic pain by repetitive spinalcord stimulation. Eur J Pain. 2017 May;21(5):804-814.McePdfHeightCaution: Product has not been fully validated for medical applications.For