JZL195-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJZL195Cat. No.: HY-15250CAS No.: 1210004-12-8分式: CHNO分量: 433.46作靶點: FAAH; MAGL作通路: Metabolic Enzyme/Protease; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 42 mg/mL (96.

2、89 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 JZL195種有效選擇的脂 酸酰胺解酶 (FAAH) 和單酰油脂肪酶 (

3、MAGL) 雙重 抑制劑，IC50s 分別為 2和 4 nM 1。IC50 & Target IC50: 2 nM (FAAH), 4 nM (MAGL) 1體外研究JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at1/2 Master of Small Molecules 您邊的抑制劑師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.體內(nèi)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