JZL195-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJZL195Cat. No.: HY-15250CAS No.: 1210004-12-8分式: CHNO分量: 433.46作靶点: FAAH; MAGL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 : 42 mg/mL (96.

2、89 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3070 mL 11.5351 mL 23.0702 mL5 mM 0.4614 mL 2.3070 mL 4.6140 mL10 mM 0.2307 mL 1.1535 mL 2.3070 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。BIOLOGICAL ACTIVITY物活性 JZL195种有效选择的脂 酸酰胺解酶 (FAAH) 和单酰油脂肪酶 (

3、MAGL) 双重 抑制剂，IC50s 分别为 2和 4 nM 1。IC50 & Target IC50: 2 nM (FAAH), 4 nM (MAGL) 1体外研究JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEconcentrations as low as 100 nM (IC50 values of 13 and 19 nM, respectively)

4、 1.JZL195 inhibits rat and human FAAH and MAGL enzymes with IC50 values in the range of 10-100 nMbased on competitive ABPP assays 1.体内研究 JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay 1.Animal Model: Male C57BL/6J mice 1Dosage: 20 mg/kgAdministration: Intrap

5、eritoneal injectionResult: Produced a much greater antinociceptive response in the tail immersion assay comparedwith inhibitors of either FAAH or MAGL alone.REFERENCES1. Long JZ, et al. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Pro

6、cNatl Acad Sci U S A. 2009 Dec 1;106(48):20270-5.2. Anderson WB, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014Jun;81:224-30.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820