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> Bardoxolone [218600-44-3]

Bardoxolone [218600-44-3]

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Référence HY-14909-1ml

Conditionnement : 10mM/1mL

Marque : MedChemExpress

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Description

Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease[1][2][3][4].
IC50 & Target

Nrf-2[1]
Cellular Effect
Cell Line Type Value Description References
HT-29 EC50
1.3 μM
Compound: 7; CDDO
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
[PMID: 33248849]
L929 EC50
> 10 μM
Compound: 7; CDDO
Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay
[PMID: 33248849]
Macrophage IC50
0.0004 μM
Compound: 4, CDDO
Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method
Antiinflammatory activity in mouse macrophages assessed as inhibition of IFN-gamma-induced nitric oxide production after 48 hrs by Griess method
[PMID: 23837912]
Macrophage IC50
0.5 nM
Compound: CDDO
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
[PMID: 21361338]
Macrophage IC50
4.3 nM
Compound: CDDO
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
Antiinflammatory activity in CD-1 mouse Macrophage assessed as inhibition of IFN-gamma induced NO production after 48 hrs by Griess reaction
[PMID: 21361338]
MCF7 EC50
0.16 μM
Compound: CDDO
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 3 days by radioactive thymidine incorporation assay
[PMID: 26177446]
RAW IC50
20 nM
Compound: CDDO
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs
Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs
[PMID: 17367124]
RAW264.7 IC50
11 nM
Compound: CDDO, Bardoxolone
Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method
Inhibition of NO production in INFgamma-stimulated mouse RAW264.7 cells measured after 24 hrs by Griess reaction method
[PMID: 21441026]
RAW264.7 IC50
16.5 nM
Compound: CDDO
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-stimulated NO production pretreated for 2 hrs before IFNgamma challenge measured after 24 hrs by Griess reaction
[PMID: 22533790]
RAW264.7 IC50
17 nM
Compound: CDDO
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction
[PMID: 21361338]
RAW264.7 IC50
23 nM
Compound: CDDO
Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay
Inhibition of iNOS in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production after 48 hrs by Griess assay
[PMID: 25965897]
RAW264.7 IC50
28.3 nM
Compound: CDDO
Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method
Antiinflammatory activity against IFN-gamma-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 24 hrs by Griess reagent method
[PMID: 20188548]
In Vitro

Bardoxolone methyl (5, 10 mg/kg) significantly decreases in levels of renal KIM-1, NGAL, TNF-α, TOS, OSI and improves deterioration in glomeruli and tubules similarly to NAC (HY-B0215) in rat kidney homogenates[3].
Bardoxolone methyl (0.3 and 1 μM, 28 h) decreases PAC-induced mitochondrial damage in the dorsal root ganglia (DRG) neuronal cell lines and increases pNRf2 intensity in the PAC-treated DRG cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bardoxolone Related Antibodies

Immunofluorescence[4]

Cell Line: PAC (10 µM)-treated DRG Cells
Concentration: 0.3 and 1 μM
Incubation Time: 28 h
Result: Increased pNRf2 intensity in PAC-treated DRG cells.
In Vivo

Bardoxolone methyl(5, 10 mg/kg) decreased the percentage of caspase-3 immunopositive cells in a dose-dependent manner in rat kidney [3].
Bardoxolone methyl (0-10 mg/kg, i.p., a single dose) results in analgesia but not sedation in rats[4].
Bardoxolone methyl [10 mg/kg, twice-daily on day 21 after the first PAC (HY-B0015) injection] decreases PAC-induced levels of pNFκB and MCP-1 by increasing pNRf2 and HO-1 in rat DRG[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
Masse moléculaire

491.66

Formule

C31H41NO4
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC1(C)CC[C@@]2(C(O)=O)[C@@]([C@](C(C=C3[C@@]4(C)CC[C@]5(16)[C@]3(C)C=C(C#N)C(C5(C)C)=O)=O)(16)[C@@]4(C)CC2)(16)C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (203.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0339 mL 10.1696 mL 20.3393 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
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