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Purity: ≥98%
Omaveloxolone (formerly known as RTA-408; Skyclarys; RTA408), an antioxidant inflammation modulator (AIM), is a 2nd generation member of the synthetic triterpenoid that can activate Nrf2 (a cytoprotective transcription factor) and inhibit NF-κB signaling. Omaveloxolone, an Nrf2 activator, enhances mitochondrial function in FA model organisms, restores redox balance, and lowers inflammation. RTA 408 activates the cytoprotective transcription factor Nrf2 after administration. After dimerizing with a small Maf protein (sMaf), Nrf2 then translocates to the nucleus and binds to the antioxidant response element (ARE). Numerous cytoprotective genes, such as sulfiredoxin 1 (Srxn1) and NAD(P)H quinone oxidoreductase 1 (NQO1), are induced by this. Omaveloxolone was given FDA approval in February 2023 to treat Friedreich's ataxia.
| Targets |
Nrf2; NF-κB
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| ln Vitro |
RTA 408 reverses IFN-mediated suppression of Gclc expression in RAW 264.7 cells and significantly upregulates the expression of Nrf2 target genes. RTA 408 inhibits growth with an average GI50 value of 260 nM in a panel of eight human tumor cell lines and triggers apoptosis. Additionally, RTA 408 inhibits NF-B and stimulates JNK in tumor cells. [1]
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| ln Vivo |
In mice with radiation-induced dermatitis, 1.0% RTA 408 markedly reduces epidermal and collagen thickening, prevents dermal necrosis and completely alleviates skin ulcers. [2] RTA 408 activates Nrf2 and induces cytoprotective genes in rat skin. [3] In mice, RTA 408 also lessens the hematopoietic acute radiation syndrome. [4]
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| Cell Assay |
Cells are plated at 3 x 103 per well in duplicate 96-well culture dishes for growth inhibition assays. The next day, one plate receives an application of RTA 408, while the other is immediately subjected to the sulforhodamine B (SRB) assay (time 0). After 72 hours of treatment with RTA 408, the cells on the plate are prepared for the SRB assay. The formula [(Ti-Tz)/(C-Tz)] x 100 is used to calculate the percentage of growth in comparison to cells treated with a vehicle. where (C) is the absorbance value from vehicle-treated wells after 72 hours, (Ti) is the absorbance value from wells treated with the drug, and (Tz) is the absorbance value at time zero. In GraphPad Prism, dose-response curves are plotted, and GI50 values are computed.
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| Animal Protocol |
Mice: Wild-type C57Bl/6 CD45.2 mice are used, which are 6–8 weeks old, for radiation survival tests. In transplantation experiments, recipients include congenic wild-type C57Bl/6 CD45.1 host mice and C57Bl/6 CD45.1/CD45.2 hybrid host mice. For vehicle control, omeveloxolone stock solutions (DMSO) are made within an hour of injection. At 24, 48, and 72 hours after irradiation, intraperitoneal administration of DMSO or omaveloxolone (17.5 mg/kg) is performed. A 250-kVp X-ray machine with a 50 cm source-to-skin distance and a 2 mm copper filter is used to administer whole-body irradiation (7-8 Gy). About 1.4 Gy/min is the dose rate.
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| References |
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| Molecular Formula |
C33H44F2N2O3
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| Molecular Weight |
554.71
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| Exact Mass |
554.33
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| Elemental Analysis |
C, 71.45; H, 8.00; F, 6.85; N, 5.05; O, 8.65
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| CAS # |
1474034-05-3
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| Appearance |
White solid powder
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| SMILES |
C[C@@]12CC[C@]3(CCC(C[C@H]3[C@H]1C(=O)C=C4[C@]2(CC[C@@H]5[C@@]4(C=C(C(=O)C5(C)C)C#N)C)C)(C)C)NC(=O)C(C)(F)F
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| InChi Key |
RJCWBNBKOKFWNY-IDPLTSGASA-N
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| InChi Code |
InChI=1S/C33H44F2N2O3/c1-27(2)11-13-33(37-26(40)32(8,34)35)14-12-31(7)24(20(33)17-27)21(38)15-23-29(5)16-19(18-36)25(39)28(3,4)22(29)9-10-30(23,31)6/h15-16,20,22,24H,9-14,17H2,1-8H3,(H,37,40)/t20-,22-,24-,29-,30+,31+,33-/m0/s1
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| Chemical Name |
N-[(4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicen-4a-yl]-2,2-difluoropropanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8027 mL | 9.0137 mL | 18.0274 mL | |
| 5 mM | 0.3605 mL | 1.8027 mL | 3.6055 mL | |
| 10 mM | 0.1803 mL | 0.9014 mL | 1.8027 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02255435 | Active Recruiting |
Drug: Placebo Drug: Omaveloxolone Capsules, 20 mg |
Friedreich Ataxia | Reata Pharmaceuticals, Inc. | January 2015 | Phase 2 |
| NCT06054893 | Not yet recruiting | Drug: Omaveloxolone | Friedreich Ataxia | Reata Pharmaceuticals, Inc. | November 2023 | Phase 1 |
| NCT03902002 | Completed | Drug: Omaveloxolone 50 mg capsules |
Hepatic Impairment | Reata Pharmaceuticals, Inc. | July 19, 2019 | Phase 1 |
| NCT03664453 | Completed | Drug: omaveloxolone | Healthy | Reata Pharmaceuticals, Inc. | July 19, 2019 | Phase 1 |
| NCT05909644 | Completed | Drug: omaveloxolone Drug: Efavirenz |
Healthy Adult Subjects | Reata Pharmaceuticals, Inc. | July 5, 2023 | Phase 1 |
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