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> Bardoxolone [218600-44-3]

Bardoxolone [218600-44-3]

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Katalog-Nummer HY-14909-1ml

Size : 10mM/1mL

Marke : MedChemExpress

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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.

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Bardoxolone Chemische Struktur

Bardoxolone Chemische Struktur

CAS. Nr. : 218600-44-3

This product is a controlled substance and not for sale in your territory.

Based on 15 publication(s) in Google Scholar

Other Forms of Bardoxolone:

  • Bardoxolone methyl In-stock
Beschreibung

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]
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.
Klinische Studie
Molekulargewicht

491.66

Formel

C31H41NO4
CAS. Nr.

218600-44-3
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(23)[C@]3(C)C=C(C#N)C(C5(C)C)=O)=O)(23)[C@@]4(C)CC2)(23)C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Lösungsmittel & Löslichkeit
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.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation

Purity: 99.14%

COA (251 KB) HNMR (199 KB) LCMS (517 KB)

Handling Instructions (2659 KB)
Verweise

  • [1]. Sun Q, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.  [Content Brief]

    [2]. Wang Y, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021 Feb 15;212:113030.  [Content Brief]

    [3]. Yasemin Teksen, et al. Bardoxolone methyl attenuates acetaminophen-induced acute kidney injury by suppressing oxidative stress, inflammation and apoptosis[J]. 2024 May 29;31(5):372–379

    [4]. Kim HK, et al. Bardoxolone Methyl Ameliorates Chemotherapy-Induced Neuropathic Pain by Activation of Phosphorylated Nuclear Factor Erythroid 2-Related Factor 2 in the Dorsal Root Ganglia. Anesth Analg. 2024 Mar 1;138(3):664-675.  [Content Brief]

  • [1]. Sun Q, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.

    [2]. Wang Y, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. Eur J Med Chem. 2021 Feb 15;212:113030.

    [3]. Yasemin Teksen, et al. Bardoxolone methyl attenuates acetaminophen-induced acute kidney injury by suppressing oxidative stress, inflammation and apoptosis[J]. 2024 May 29;31(5):372–379

    [4]. Kim HK, et al. Bardoxolone Methyl Ameliorates Chemotherapy-Induced Neuropathic Pain by Activation of Phosphorylated Nuclear Factor Erythroid 2-Related Factor 2 in the Dorsal Root Ganglia. Anesth Analg. 2024 Mar 1;138(3):664-675.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0339 mL 10.1696 mL 20.3393 mL 50.8481 mL
5 mM 0.4068 mL 2.0339 mL 4.0679 mL 10.1696 mL
10 mM 0.2034 mL 1.0170 mL 2.0339 mL 5.0848 mL
15 mM 0.1356 mL 0.6780 mL 1.3560 mL 3.3899 mL
20 mM 0.1017 mL 0.5085 mL 1.0170 mL 2.5424 mL
25 mM 0.0814 mL 0.4068 mL 0.8136 mL 2.0339 mL
30 mM 0.0678 mL 0.3390 mL 0.6780 mL 1.6949 mL
40 mM 0.0508 mL 0.2542 mL 0.5085 mL 1.2712 mL
50 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0170 mL
60 mM 0.0339 mL 0.1695 mL 0.3390 mL 0.8475 mL
80 mM 0.0254 mL 0.1271 mL 0.2542 mL 0.6356 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5085 mL
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Bardoxolone Related Classifications

  • NF-κB Apoptosis
  • Keap1-Nrf2 Necroptosis
Help & FAQs

Keywords:

Bardoxolone218600-44-3CDDO RTA 401RTA401RTA 401RTA-401Keap1-Nrf2Necroptosischronic kidney diseaseHT-29 cellsnecroptosisNrf2 activatorantioxidant systeminflammatory cytokinesapoptosisrat kidneymitochondrial damageanalgesic effectneuropathic painInhibitorinhibitorinhibit

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