Companies
MedChemExpress LLC (MCE)
Products
MedChemExpress - Model Bardoxolone ...

MedChemExpress - Model Bardoxolone methyl - 218600-53-4

Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.

Bardoxolone methyl

MCE China：Bardoxolone methyl

Brand：MedChemExpress (MCE)

Cat. No.HY-13324

CAS：218600-53-4

Synonyms：RTA 402; NSC 713200; CDDO Methyl ester

Purity：98.92%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.

In Vivo：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].

Animal Administration：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.

IC50 & Target：Nrf2[1] Cellular Effect Cell Line Type Value Description References

References：

[1]. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Aug 2. [Content Brief]

[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. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。