甲基巴多索隆作用机制 - Medchemexpress - MCE中国

1、Product Data SheetBardoxolone (methyl)Cat. No.: HY-13324CAS No.: 218600-53-4分式: CHNO分量: 505.69作靶点: Keap1-Nrf2; Autophagy; Apoptosis; Ferroptosis作通路: NF-B; Autophagy; Apoptosis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 : 25 mg/mL (49.44 mM; Need ultrasonic)H2

2、O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.9775 mL 9.8875 mL 19.7750 mL5 mM 0.3955 mL 1.9775 mL 3.9550 mL10 mM 0.1977 mL 0.9887 mL 1.9775 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1

3、个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.94 mM); Clear solution此案可获得 2.5 mg/mL (

4、4.94 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.94 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (4.94 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1

5、 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) 炎活性，作为 Nrf2 通路的激活剂和 NF-B 途径的抑制剂。种合成的三萜类化合物，具有潜在的抗肿瘤和抗IC & Target Nrf21体内研究 Bardoxolone methyl (30 mg/kg, p.o.) decreases renal expression of megalin but not cubi

6、lin, increases creatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets in cynomolgus monkeys1 . Bardoxolone methyl induces overall favorable effects on the heart via its improvement in eGFR in both animalmodels and clinical trials2.PROTOCOLAnimal Two se

7、parate 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 oil as thevehicle, at 5, 30, and 300 mg/kg once daily for 12 months in a GLP environment. Ob

8、servations for morbidity,mortality, injury, and the availability of food and water are conducted twice daily for all animals. Clinical observationsand body weights are conducted and recorded weekly. Weight data are analyzed by calculating the area under theweight versus time curve using the linear t

9、rapezoidal method. Blood samples for clinical chemistry evaluations arecollected 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 dose group are allowed to recover for 4 weeks.MCE has not independently

10、 confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Pharmacol Exp Ther. 2020 Apr;373(1):149-159. 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.See more customer val

11、idations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2.2. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effects of bardoxolonemethyl. Drug Des Devel Ther. 2012;6:141-9.Page 2 of 3 www.MedChemEMcePdfHeightCaution: Product has not been fully vali