Page last updated: 2024-11-13

rta 408

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

omaveloxolone: has both anti-inflammatory and radiation protective activities [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71811910
CHEMBL ID4303525
SCHEMBL ID15349371
MeSH IDM000595603

Synonyms (37)

Synonym
HY-12212
omaveloxolone
skyclarys
gtpl7573
rta 408
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
rta-408 ,
unii-g69z98951q
n-(11-cyano-2,2,6a,6b,9,9,12a-heptmethyl-10,14-dioxo-1,3,4,5,6a,6b,7,8,8a,9,10,12a,14,14a,14b-hexadecahydro-2h-picen-4a-yl)-2-2-difluoropropionamide
SCHEMBL15349371
propanamide, n-(2-cyano-3,12-dioxo-28-noroleana-1,9(11)-dien-17-yl)-2,2-difluoro-
1474034-05-3
omaveloxolone [who-dd]
G69Z98951Q ,
omaveloxolone [inn]
omaveloxolone [usan]
n-((4as,6ar,6bs,8ar,12as,14ar,14bs)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide
EX-A541
rta408
D10964
omaveloxolone (usan/inn)
n-(2-cyano-3,12-dioxo-28-noroleana-1,9(11)-dien-17-yl)-2,2-difluoropropanamide
mfcd28167769
DB12513
BS-15146
Q21098900
rta408; rta408; rta-408;nrf1-activator-1
BCP28609
CHEMBL4303525
nrf1-activator-1
AKOS037648676
DTXSID101138251
rjcwbnbkokfwny-idpltsgasa-n
omaveloxolona
omaveloxolonum
AC-37100
n-((4as,6ar,6bs,8ar,12as,14ar,14bs)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-hexadecahydropicen-4a(2h)-yl)-2,2-difluoropropanamide

Research Excerpts

Overview

RTA 408 is a member of the synthetic oleanane triterpenoid class of compounds. It is known to potently activate the cytoprotective transcription factor Nrf2.

ExcerptReferenceRelevance
"RTA 408 is a member of the synthetic oleanane triterpenoid class of compounds known to potently activate the cytoprotective transcription factor Nrf2. "( Topical application of the synthetic triterpenoid RTA 408 activates Nrf2 and induces cytoprotective genes in rat skin.
Lee, CY; Meyer, CJ; Proksch, JW; Reisman, SA; Ward, KW, 2014
)
2.1

Treatment

RTA 408 treats and corrects the irregularity in redox balance mechanisms involving Nrf2. RTA 408 pretreatment significantly protected cells from oxidative stress-induced GSH loss, GSSG formation and decreased ROS production.

ExcerptReferenceRelevance
"RTA 408 treatment attenuated the morphological changes caused by cerebral vasospasm."( Mechanisms and therapeutic implications of RTA 408, an activator of Nrf2, in subarachnoid hemorrhage-induced delayed cerebral vasospasm and secondary brain injury.
Lin, CL; Lin, SH; Tsai, TH; Tsai, YC; Wu, CH; Yang, SF, 2020
)
1.54
"RTA 408-treated diabetic wounds upregulated Nrf2 and downstream antioxidant genes, and exhibited well-vascularized granulation tissue that aided in re-epithelialization."( Targeted Nrf2 activation therapy with RTA 408 enhances regenerative capacity of diabetic wounds.
Abdou, S; Ceradini, DJ; Cohen, JM; David, JA; Ellison, T; Gomez-Viso, A; Kim, C; Lam, G; Rabbani, PS; Sultan, D; Thomson, J; Waqas, B, 2018
)
1.47
"RTA 408 treats and corrects the irregularity in redox balance mechanisms involving Nrf2, in an avenue not explored previously for treatment of diabetic wounds and tissue regeneration."( Targeted Nrf2 activation therapy with RTA 408 enhances regenerative capacity of diabetic wounds.
Abdou, S; Ceradini, DJ; Cohen, JM; David, JA; Ellison, T; Gomez-Viso, A; Kim, C; Lam, G; Rabbani, PS; Sultan, D; Thomson, J; Waqas, B, 2018
)
1.47
"RTA 408 pretreatment significantly protected cells from oxidative stress-induced GSH loss, GSSG formation and decreased ROS production."( The novel triterpenoid RTA 408 protects human retinal pigment epithelial cells against H2O2-induced cell injury via NF-E2-related factor 2 (Nrf2) activation.
Clark, AF; Jann, J; Liu, X; Pang, IH; Ward, K; Wu, H; Xavier, C, 2016
)
1.47
"Pretreatment with RTA 408 attenuated the IL-1β-induced c-Jun phosphorylation, mRNA expression, and promoter activity."( RTA 408 Inhibits Interleukin-1β-Induced MMP-9 Expression via Suppressing Protein Kinase-Dependent NF-κB and AP-1 Activation in Rat Brain Astrocytes.
Hsiao, LD; Jou, MJ; Lin, CC; Yang, CC; Yang, CM, 2019
)
2.28

Toxicity

ExcerptReferenceRelevance
"In the MOXIe trial, omaveloxolone significantly improved neurological function compared to placebo and was generally safe and well tolerated."( Safety and Efficacy of Omaveloxolone in Friedreich Ataxia (MOXIe Study).
Boesch, S; Chin, MP; Corti, M; Delatycki, MB; Giunti, P; Goldsberry, A; Hoyle, JC; Lynch, DR; Mariotti, C; Mathews, KD; Meyer, CJ; Nachbauer, W; O'Grady, M; Perlman, S; Subramony, SH; Wilmot, G; Zesiewicz, T, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacodynamic (PD) evaluations in monkeys consisted of Nrf2 target gene mRNA expression in peripheral blood mononuclear cells (PBMCs), liver, lung, and brain."( Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates.
Gahir, SS; Lee, CI; Proksch, JW; Reisman, SA; Sakamoto, M; Ward, KW, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency1.31370.00529.466132.9993AID1347411
Interferon betaHomo sapiens (human)Potency1.31370.00339.158239.8107AID1347411
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (30)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID1728767Anti-necroptotic activity in mouse L929 cells assessed as inhibition of TNFalpha/Z-VAD-fmk (TZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors.
AID1728762Anti-necroptotic activity in human HT-29 cells assessed as inhibition of TNFalpha/SM-164/Z-VAD-fmk (TSZ)-induced necroptosis by measuring increase in cell viability measured after 12 hrs by celltiter-glo luminescent cell viability assay2021European journal of medicinal chemistry, Feb-15, Volume: 212Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors.
AID1347414qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Secondary screen by immunofluorescence2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (33)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's15 (45.45)24.3611
2020's18 (54.55)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.25

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.25 (24.57)
Research Supply Index3.69 (2.92)
Research Growth Index4.76 (4.65)
Search Engine Demand Index34.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.25)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (18.18%)5.53%
Reviews2 (6.06%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (75.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]