ITX5061 - p38 MAPK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEITX5061Cat. No.: HY-19900CAS No.: 1252679-52-9分式: CHClNOS分量: 620.16作靶点: p38 MAPK作通路: MAPK/ERK Pathway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 : 83.3 mg/mL (134.32 mM)* means soluble, b

2、ut saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.6125 mL 8.0624 mL 16.1249 mL5 mM 0.3225 mL 1.6125 mL 3.2250 mL10 mM 0.1612 mL 0.8062 mL 1.6125 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 ITX5061个 II 型 p38 MAPK 抑制剂，也是清道夫受体 B1 (SR-B1) 的拮抗剂。IC50 & Tar

3、get p38 MAPK, SR-B1 1体内研究ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).Treatment of ITX5061 (30 mg/kg/day) for mice results in a 50% increase in HDL-C levels compare to1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEbaseline. ApoA-I levels are mo

4、derately (+15 %) but significantly increased in ITX5061-treated HuAITg mice,compare to mice receive vehicle. ITX5061 significantly decreases HDL-CE catabolism with an FCR of1.860.40 pools/d vs 2.470.26 pools/d in the control group (P3H CE in the liver is significantly lower inITX5061-treated mice in

5、dicating that increased HDL-CE levels are due to reduced uptake by the liver 1.PROTOCOLAnimal Atherosclerosis studies are conducted in F1 hybrid C57BL/6DBA/1 Ldlr+/- mice fed the Paigen diet, which isAdministration 1 high-fat/cholesterol/bile salt diet containing 1.25% cholesterol, 7.5% cocoa butter

6、, and 0.5% cholic acid. For18 weeks, the mice are put on the Paigen diet with or without ITX5061 at 0.037 %. CETP expression isinduced by injection of adeno-associated virus (AAV)8 TBG human CETP vector two weeks before startingthe Paigen diet. Doses of virus are given by IP injection 1.MCE has not

7、independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Masson D, et al. Increased HDL cholesterol and apoA-I in humans and mice treated with a novel SR-BI inhibitor. Arterioscler ThrombVasc Biol. 2009 Dec;29(12):2054-60.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use