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Bardoxolone

Cat. No. M5238

Bardoxolone Structure

Synonym: RTA 402; CCDO

Size Price Availability Quantity
5mg USD 95 In stock
10mg USD 135 In stock
50mg USD 375 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 491.66
Formula C31H41NO4
CAS Number 218600-44-3
Purity >99%
Solubility 21 mg/mL in DMSO
Storage at -20°C
References

Risk factors for heart failure in patients with type 2 diabetes mellitus and stage 4 chronic kidney disease treated with bardoxolone methyl.
Chin MP, et al. J Card Fail. 2014 Dec;20(12):953-8. PMID: 25307295.

Mechanisms contributing to adverse cardiovascular events in patients with type 2 diabetes mellitus and stage 4 chronic kidney disease treated with bardoxolone methyl.
Chin MP, et al. Am J Nephrol. 2014;39(6):499-508. PMID: 24903467.

Bardoxolone methyl in type 2 diabetes and stage 4 chronic kidney disease.
de Zeeuw D, et al. N Engl J Med. 2013 Dec 26;369(26):2492-503. PMID: 24206459.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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