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Bardoxolone-methyl-(NSC-713200)-Keap1-Nrf2-Activator-MedChemExpress

Bardoxolone methyl

体内研究

Bardoxolone methyl (30 mg/kg, p.o.) decreases renal expression of megalin but not cubilin, increases creatinine clearance and urinary albumin-to-creatinine ratios, and induces Nrf2 cytoprotective targets in cynomolgus monkeys [1]. Bardoxolone methyl induces overall favorable effects on the heart via its improvement in eGFR in both animal models and clinical trials [2].

PROTOCOL

Animal

Administration [1]

Two separate in-life studies are conducted in cynomolgus monkeys. In one study, cynomolgus monkeys

(n=9/gender/dose group) are administered amorphous bardoxolone methyl by oral gavage, using sesame oil as the vehicle, at 5, 30, and 300 mg/kg once daily for 12 months in a GLP environment. Observations for morbidity, 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 by calculating the area under the weight versus time curve using the linear trapezoidal method. Blood samples for 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 dose group are allowed to recover for 4 weeks.MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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REFERENCES

[1]. 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 bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9.

McePdfHeight

Caution: Product has not been fully validated for medical applications. For research use only.

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Master of Small Molecules — 您?边的抑制剂?师

? Toxicol Lett . 2016 Sep 30;259:52-59.

? J Histochem Cytochem . 2016 Apr;64(4):237-55.? bioRxiv . 2019 Mar.

? School of Medicine . University of Wollongong. 2017 Dec.

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