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Bardoxolone

Cat. No. M5238
Bardoxolone Structure
Synonym:

RTA 402; CCDO

Size Price Availability Quantity
1mg USD 36  USD36 In stock
5mg USD 80  USD80 In stock
10mg USD 110  USD110 In stock
50mg USD 175  USD175 In stock
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Quality Control & Documentation
Biological Activity

In vitro: Bardoxolone exhibits potent inhibitory activities against production of nitric oxide induced by interferon-Ƴ in mouse macrophages with IC50 of 0.1 nM. Bardoxolone Methyl decreases the viability of leukemic HL-60, KG-1, and NB4 cells with IC50 of 0.4, 0.4, and 0.27 μM, respectively. CDDO-Me induces pro-apoptotic Bax protein, inhibits the activation of ERK1/2, and it blocks Bcl-2 phosphorylation, which contributes to the induction of apoptosis. Bardoxolone Methyl potently inhibits both constitutive and inducible NF-kappaB activated by TNF, interleukin (IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, and cigarette smoke.

In vivo: Bardoxolone (60 mg/kg) reduces the number, size, and severity of lung tumors in vivo. Bardoxolone Methyl significantly reduces the in vivo inflammatory cytokine response following LPS challenge, induces HO-1 protein expression in the spleen, and protects mice against lethal-dose LPS.

Protocol (for reference only)
Cell Experiment
Cell lines HL-60, KG-1, and NB4 cells
Preparation method Leukemic cell lines are cultured at a density of 3.0 × 10^5 cells/mL, and AML mononuclear cells are cultured at 5 × 10^5 cells/mL in the presence or absence of indicated concentrations of CDDO-Me. Appropriate amounts of DMSO (final concentration less than 0.05%) are included as control. For cytotoxicity studies, 1 μM ara-C is added to the cultures. After 24 to 72 hours, viable cells are counted with the trypan blue dye exclusion method using a hematocytometer.
Concentrations ~5 μM
Incubation time 72 hours
Animal Experiment
Animal models Female A/J mice are injected i.p. with vinyl carbamate.
Formulation DMSO
Dosages ~60 mg/kg
Administration Oral gavage
Chemical Information
Molecular Weight 491.66
Formula C31H41NO4
CAS Number 218600-44-3
Solubility (25°C) 21 mg/mL in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Chin MP, et al. J Card Fail. Risk factors for heart failure in patients with type 2 diabetes mellitus and stage 4 chronic kidney disease treated with bardoxolone methyl.

[2] Chin MP, et al. Am J Nephrol. Mechanisms contributing to adverse cardiovascular events in patients with type 2 diabetes mellitus and stage 4 chronic kidney disease treated with bardoxolone methyl.

[3] de Zeeuw D, et al. N Engl J Med. Bardoxolone methyl in type 2 diabetes and stage 4 chronic kidney disease.

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Keywords: Bardoxolone, RTA 402; CCDO supplier, IκB/IKK, inhibitors, activators


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