AA26-9 _Phospholipase 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAA26-9Cat. No.: HY-18522CAS No.: 1312782-34-5分式: CHNO分量: 166.18作靶点: Phospholipase作通路: Metabolic Enzyme/Protease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 (601.76 mM; Need ult

2、rasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 6.0176 mL 30.0879 mL 60.1757 mL5 mM 1.2035 mL 6.0176 mL 12.0351 mL10 mM 0.6018 mL 3.0088 mL 6.0176 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，

3、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 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (15.04 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (15.04 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (15.04 mM)

4、; Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 AA26-9有效谱的丝氨酸解酶抑制剂。体外研究 AA26-9 is synthesized based on a piperazine scaffold shown previously to inhibit serine hydrolases in thecontext of p-nitrophenoxy carbamate. AA26-9-inhibited enzymes originated from diver

5、se functionalsubclasses of serine hydrolases, including lipases/phospholipases (AADACL1, ABHD6, ESD, FAAH,PAFAH2, LYPLA3), peptidases (APEH, PRCP, CTSA), thioesterases (LYPLA1, LYPLA2), anduncharacterized enzymes (ABHD11, ABHD13, BAT5). AA26-9 inhibits one of its enzyme targets LYPLA1 bycovalent car

6、bamoylation of the enzymes serine nucleophile (S114). AA26-9 inhibits 1/3 of the over 40 serinehydrolase found in T-cells 1.PROTOCOLCell Assay 1 Cells are cultured with 20 M inhibitor AA26-9 or DMSO as a control for 4 h, lysed, separated into solubleand analyzed by competitive gel-based ABPP 1.MCE h

7、as not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Adibekian A, et al. Click-generated triazole ureas as ultrapotent in vivo-active serine hydrolase inhibitors. Nat Chem Biol. 2011 May15;7(7):469-78.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use