1. NF-κB
  2. Keap1-Nrf2
    NF-κB

RTA-408 (Synonyms: Omaveloxolone)

Cat. No.: HY-12212 Purity: 98.96%
Data Sheet SDS Handling Instructions

RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB.

For research use only. We do not sell to patients.
RTA-408 Chemical Structure

RTA-408 Chemical Structure

CAS No. : 1474034-05-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO $159 In-stock
5 mg $130 In-stock
10 mg $220 In-stock
50 mg $750 In-stock
100 mg $1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-κB. IC50 value: Target: Nrf2 activator Mice were irradiated (10 Gy/day) on days 0-2 and 5-7, and RTA 408 (0.01%, 0.1% and 1.0%) was topically applied once daily starting on day 5 or up to day 40. Dermatitis severity was evaluated using a scale ranging from 0 (normal) to 5 (frank ulceration), as well as histologically. The mRNA expression of Nrf2 and NF-κB target genes in skin was also evaluated. RTA 408 (0.01%, 0.1% and 1.0%) reduced the percentage of animal-days with scores ≥2 by 11%, 31% and 55% and scores ≥3 by 16%, 60% and 80%, respectively [1]. RTA 408 (0.1, 1.0, or 3.0%) was applied topically to the shaved skin of male Sprague-Dawley rats twice daily for 4 days and once on Day 5. Topical application of RTA 408 resulted in transdermal penetration, with low but dose-dependent plasma exposure with AUC(0-24 h) values of 3.6, 26.0, and 41.1 h ng/mL for the 0.1, 1.0, and 3.0% doses, respectively [2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02029729 Reata Pharmaceuticals, Inc.|AbbVie Metastatic or Incurable Non-small Cell Lung Cancer|Relapsed, Refractory Melanoma December 2013 Phase 1
NCT02128113 Reata Pharmaceuticals, Inc.|AbbVie Corneal Endothelial Cell Loss|Ocular Pain|Ocular Inflammation|Cataract Surgery May 2014 Phase 2
NCT02142959 Reata Pharmaceuticals, Inc.|AbbVie Breast Cancer June 2014 Phase 2
NCT02259231 Reata Pharmaceuticals, Inc. Melanoma|Unresectable (Stage III) Melanoma|Metastatic (Stage IV) Melanoma October 2014 Phase 1|Phase 2
NCT02255422 Reata Pharmaceuticals, Inc.|AbbVie MItochondrial Myopathies April 2015 Phase 2
NCT02255435 Reata Pharmaceuticals, Inc.|AbbVie|Friedreich's Ataxia Research Alliance Friedreich Ataxia January 2015 Phase 2
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References
Molecular Weight

554.71

Formula

C₃₃H₄₄F₂N₂O₃

CAS No.

1474034-05-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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RTA-408
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HY-12212
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