| Size | Price | |
|---|---|---|
| 50mg | ||
| 100mg | ||
| 250mg |
| ln Vitro |
Novel synthetic triterpenoid, bardoxolone methyl, is an antioxidant inflammation modulator that potently induces Nrf2 and inhibits Janus-activated kinase/STAT signaling, NF-κB. It has been demonstrated that bardoxolone methyl causes cancer cell lines to differentiate, stop growing, and undergo apoptosis[2].
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| ln Vivo |
Although the groups' mRNA expression is similar, kidney sections from the bardoxolone methyl-treated monkeys show reduced megalin protein expression. Densitometry analyses validate the observed reduction in megalin protein expression, revealing a significant decrease in megalin protein expression in the monkey kidney upon administration of Bardoxolone methyl. Both the mRNA and protein expression of cubilin in the kidney are unaffected by the administration of bardoxolone methyl. On day 28, the creatinine clearance of monkeys given Bardoxolone methyl was considerably different from that of baseline and animals given a vehicle treatment. Urinary albumin-to-creatinine ratios (UACRs), as measured from 24-hour urine collections, are significantly higher after 28 days of Bardoxolone methyl administration in comparison to animals receiving vehicle. Notably, UACRs rose by 27.9% in monkeys treated with bardoxolone methyl and decreased by 53.3% in animals treated with a vehicle[3]. For 21 weeks, male C57BL/6J mice are either fed a low-fat diet (LFD), only a high-fat diet (HFD), or oral BARD during HFD feeding (HFD/BARD). HFD mice show a significant increase in F4/80 crown-like structures (+95%; p<0.001) in comparison to LFD mice, which is effectively prevented by BARD (−50%; p<0.01). Similarly, compared to LFD mice and HFD/BARD mice, the number of F4/80 interstitial macrophages in HFD mice is significantly higher by 98% (p<0.001) and 32% (p<0.01), respectively[4].
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| References |
[1]. McCullough PA, et al. Cardiac and renal function in patients with type 2 diabetes who have chronic kidney disease: potential effectsof bardoxolone methyl. Drug Des Devel Ther. 2012;6:141-9.
[2]. Hong DS, et al. A phase I first-in-human trial of bardoxolone methyl in patients with advanced solid tumors and lymphomas. Clin Cancer Res. 2012 Jun 15;18(12):3396-406. [3]. Reisman SA, et al. Bardoxolone Methyl Decreases Megalin and Activates Nrf2 in the Kidney. J Am Soc Nephrol. 2012 Oct;23(10):1663-73. [4]. Dinh CH, et al. Bardoxolone Methyl Prevents Mesenteric Fat Deposition and Inflammation in High-Fat Diet Mice. ScientificWorldJournal. 2015;2015:549352 |
| Molecular Formula |
C31H41NO4
|
|---|---|
| Molecular Weight |
491.672
|
| Exact Mass |
491.3036
|
| CAS # |
218600-44-3
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| SMILES |
O=C1C([H])=C2C3(C([H])=C(C#N)C(C(C([H])([H])[H])(C([H])([H])[H])C3([H])C([H])([H])C([H])([H])[C@@]2(C([H])([H])[H])[C@]2(C([H])([H])[H])C([H])([H])C([H])([H])C3(C(=O)O[H])C([H])([H])C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[C@@]3([H])C21[H])=O)C([H])([H])[H]
|
| Synonyms |
BardoxoloneCDDO RTA-401 RTA 401RTA401
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~203.39 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0339 mL | 10.1694 mL | 20.3388 mL | |
| 5 mM | 0.4068 mL | 2.0339 mL | 4.0678 mL | |
| 10 mM | 0.2034 mL | 1.0169 mL | 2.0339 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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