Bardoxolone-methyl-NSC-713200-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBardoxolone methylCat. No.: HY-13324CAS No.: 218600-53-4Synonyms: NSC 713200; RTA 402; CDDO Methyl ester分式: CHNO分量: 505.69作靶点: Keap1-Nrf2; Autophagy作通路: NF-B; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-2

2、0C 1 month溶解性数据体外实验 DMSO : 75 mg/mL (148.31 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 3.25 mg/mL (6.43 mM); Suspended solution; Need ultrasonic2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.25 mg/mL (6.43 mM); Suspended solution; Need ultrasonic1/3 Master

3、 of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3.25 mg/mL (6.43 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester)种合成的三萜类化合物，具有潜在的抗肿瘤和抗炎活性，作为 Nrf2 通路的激活剂和 NF-B 途径的抑制剂。IC50 & Target Nrf2 1体内研究 Bardoxolone methyl

4、 (30 mg/kg, p.o.) decreases renal expression of megalin but not cubilin, increasescreatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets incynomolgus monkeys 1. Bardoxolone methyl induces overall favorable effects on the heart via itsimprovement in eGF

5、R in both animal models and clinical trials 2.PROTOCOLAnimal Two separate in-life studies are conducted in cynomolgus monkeys. In one study, cynomolgus monkeysAdministration 1 (n=9/gender/dose group) are administered amorphous bardoxolone methyl by oral gavage, using sesame oilas the vehicle, at 5,

6、30, and 300 mg/kg once daily for 12 months in a GLP environment. Observations formorbidity, mortality, injury, and the availability of food and water are conducted twice daily for all animals.Clinical observations and body weights are conducted and recorded weekly. Weight data are analyzed bycalcula

7、ting the area under the weight versus time curve using the linear trapezoidal method. Blood samplesfor clinical chemistry evaluations are collected from all animals pretest and from all animals prior to interim (6-month) and terminal (12-month) necropsies. An additional group of monkeys for each dos

8、e group are allowedto recover for 4 weeks.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Toxicol Lett. 2016 Sep 30;259:52-59. J Histochem Cytochem. 2016 Apr;64(4):237-55. Toxicon. 2019 Jul 26. pii: S0041-0101(19)30417-9. bioRxiv. 2019 Mar.

9、School of Medicine. University of Wollongong. 2017 Dec.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effects ofbardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9.McePdfHeightCaution: Product has not been fully validated