LR-90-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELR-90Cat. No.: HY-76383CAS No.: 245075-84-7分式: CHClNO分量: 709.57作靶点: Others作通路: Others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 (140.93 mM)H2O : 40% PEG300 5% Tween-80 45% sa

2、lineSolubility: 2.5 mg/mL (3.52 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.52 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 LR-90晚期糖 化终产物 (advanced glycation end product (AGE) 抑制剂，能够抑制单核细胞的炎症反应 1。LR-90 也可于糖尿病动物模型研究 2。IC

3、50 & Target AGE 1体外研究 LR-90 (0, 25, 50, 100, and 200 M) inhibits RAGE, MCP-1, COX-2, IP-10 and NOX2 mRNA expression inTHP-1 cells in a dose-dependent manner, after pretreatment 1 h befor S100b stimulatation for 4 hours 1.LR-90 (0, 25, 50, 100, and 200 M) dose-dependently and significantly blocks THP

4、-1 cells adherence toendothelial cells after pretreatment 1 h befor S100b stimulatation for 24 hours 1.LR-90 (0, 25, 50, 100, and 200 M, for 24 hours) shows no effect on the cell viability of THP-1 cells 1.Cell Viability Assay 1Cell Line: THP-1 cellsConcentration: 0, 25, 50, 100, and 200 MIncubation

5、 Time: 24 hoursResult: Showed no cytotoxicity to THP-1 cells.RT-PCR 1Cell Line: THP-1 cellsConcentration: 0, 25, 50, 100, and 200 MIncubation Time: One hour before S100b addition for 4 hoursResult: Dose-dependently inhibited mRNA expression of RAGE, MCP-1, COX-2, IP-10, andNOX2 stimulated with S100b

6、.体内研究LR-90 (50 mg/L, p.o. for 27 weeks) significantly reduces plasma lipids, modestly affects hyperglycaemia inZDF rats 2.LR-90 (50 mg/L) decreases renal AGE, AGER and lipid peroxidation 2.Animal Model: Male ZDF rats (13 to 40 weeks) 2Dosage: 50 mg/LAdministration: P.O. for 27 weeksResult: Significa

7、ntly reduced plasma triacylglycerol and cholesterol by -55% and -30%,respectively. Modestly affected hyperglycaemia and blood pressure. Lowered the body2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEweight.REFERENCES1. Figarola JL, et al. Anti-inflammatory effects of the advanced glycation end pro

8、duct inhibitor LR-90 in human monocytes. Diabetes. 2007Mar;56(3):647-55.2. Figarola JL, et al. LR-90 prevents dyslipidaemia and diabetic nephropathy in the Zucker diabetic fatty rat. Diabetologia. 2008May;51(5):882-91.McePdfHeightCaution: Product has not been fully validated for medical applications.For