Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ACTIVATOR
Mechanism of action
Activator of nuclear factor; erythroid 2 like 2
Product Description
Information
Omaveloxolone (RTA-408) Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
Targets
NF-κB ; Nrf2
In vitro
RTA 408 potently increases expression of Nrf2 target genes and reverses IFNγ-mediated suppression of Gclc expression in RAW 264.7 cells. In a panel of eight human tumor cell lines, RTA 408 inhibits growth with an average GI50 value of 260 nM and induces apoptosis. RTA 408 also inhibits NF-κB and activates JNK in tumor cells.
In 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. In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. RTA 408 also mitigates hematopoietic acute radiation syndrome in mice.
1.Reisman SA, Lee CY, Meyer CJ, Proksch JW, Ward KW. (2014) Topical application of the synthetic triterpenoid RTA 408 activates Nrf2 and induces cytoprotective genes in rat skin.. Arch Dermatol Res, 306 (5):(447-54). [PMID:24362512]
2.Reisman SA, Lee CY, Meyer CJ, Proksch JW, Sonis ST, Ward KW. (2014) Topical application of the synthetic triterpenoid RTA 408 protects mice from radiation-induced dermatitis.. Radiat Res, 181 (5):(512-20). [PMID:24720753]
3.Reisman SA, Gahir SS, Lee CI, Proksch JW, Sakamoto M, Ward KW. (2019) Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates.. Drug Des Devel Ther, 13 (3):(1259-1270). [PMID:31118567]
4.Ghanekar SD, Miller WW, Meyer CJ, Fenelon KJ, Lacdao A, Zesiewicz TA. (2019) Orphan Drugs In Development For The Treatment Of Friedreich's Ataxia: Focus On Omaveloxolone.. Degener Neurol Neuromuscul Dis, 9 (3):(103-107). [PMID:31686946]
5.Profeta V, McIntyre K, Wells M, Park C, Lynch DR. (2023) Omaveloxolone: an activator of Nrf2 for the treatment of Friedreich ataxia.. Expert Opin Investig Drugs, 32 (1):(5-16). [PMID:36708320]
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