Leonurine-hydrochloride-SCM-198-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELeonurine hydrochlorideCat. No.: HY-N0741ACAS No.: 24735-18-0Synonyms: SCM-198 hydrochloride分式: CHClNO分量: 347.79作靶点: Autophagy作通路: Autophagy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 : 3

2、1 mg/mL (89.13 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8753 mL 14.3765 mL 28.7530 mL5 mM 0.5751 mL 2.8753 mL 5.7506 mL10 mM 0.2875 mL 1.4376 mL 2.8753 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 Leonurine hydrochloride从

3、 Herba leonuri 中分离到的物碱，具有抗氧化、抗炎活性。体外研究Leonurine (0, 5, 10, 20, 40, 80 M) causes diminution in lipid accumulation, cellular cholesterol content,including total cholesterol (TC), free cholesterol (FC) and cholesteryl ester (CE), and increase in apoA-I- orHDL-mediated cholesterol efflux after treatment

4、 for 24 h. Leonurine also significantly and dose-dependently1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEincreases the expressions of ABCA1 and ABCG1 at the mRNA and protein levels in human THP-1macrophages, and such effect is involved in PPAR 1. Leonurine hydrochloride (LH) shows protective eff

5、ecton cell viability of HepG2 and HL-7702 cells incubated with palmitic acid (PA) of free fatty acid (FFA) for 24h.Leonurine hydrochloride (125, 250, 500M) improves cellular lipid accumulation in HepG2 and HL-7702 cellsvia activating AMPK/SREBP1 pathway 2. Leonurine (5, 10, 20M) inhibits the express

6、ion of iNOS, COX-2,PGE2, NO, TNF-, and IL-6 in IL-1-induced human chondrocytes, suppresses ECM degradation in humanOA chondrocytes, and blocks IL-1-induced PI3K and Akt phosphorylation in a dose-dependent manner 3.体内研究 Leonurine (10 mg/kg/d, p.o.) significantly increases the expressions of PPAR, LXR

7、, ABCA1 and ABCG1,and decreases both TG and TC levels in serum of mice 1. Leonurine hydrochloride (50, 100, 200 mg/kg)improves intracellular lipid accumulation via activating AMPK/SREBP1 pathway, enhances biochemicalparameters, reduces hepatic lipoperoxide and increases antioxidant levels in mice 2.

8、 Leonurine (20mg/kg,p.o.) ameliorates osteoarthritis development in mouse DMM model 3.PROTOCOLCell Assay 2 MTT assay is performed to study the cytotoxic effects of Leonurinein HepG2 and HL-7702 cells. Briefly,HepG2 and HL-7702 cells are seeded for 24h at the density of 3104 cells/well in 96-well pla

9、tes. After 24hincubation, cells are treated with different concentrations of Leonurine (0-1000M) and the control group istreated with only DMEM for 24h at 37C in 5% CO2 incubator. Then, these cells are treated with MTTsolution (5mg/mL) for further 4h. After 4h incubation, DMEM containing MTT solutio

10、n is discarded. Cells arethen dissolved by adding DMSO (200L) to each well and the solutions are mixed thoroughly for 5min.Finally, the absorbance is determined at 570nm with a microplate reader 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal M

11、iceApoE-/- mice (male, eight-week old) are fed a chow diet for 2 weeks, apoE-/- mice are randomly dividedAdministration 1 into several groups (n=15/group). Mice in the Leonurine group are intragastrically administered withLeonurine (10 mg/kg/d) every day and continued for 8 weeks. The control group

12、is fed with an equal volumeof PBS. At week 16, mice are euthanized, followed by collecting the blood and tissue samples for furtheranalyses 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Jiang T, et al. Leonurine Prevents Atherosclerosis

13、 Via Promoting the Expression of ABCA1 and ABCG1 in a Ppar/Lxr SignalingPathway-Dependent Manner. Cell Physiol Biochem. 2017;43(4):1703-1717.2. Zhang L, et al. Novel hepatoprotective role of Leonurine hydrochloride against experimental non-alcoholic steatohepatitis mediated viaAMPK/SREBP1 signaling pathway. Biomed Pharmacother. 2018 Dec 7;110:571-581.3. Hu ZC, et al. Inhibition of PI3K/Akt/NF-B signaling with leonurine for ameliorating the progression of osteoarthritis: In vitro and in vivostudies. J Cell Physiol. 2018 No