Page last updated: 2024-12-08

tempol

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

Cross-References

ID SourceID
PubMed CID137994
CHEMBL ID607023
CHEBI ID180664
MeSH IDM0042155

Synonyms (64)

Synonym
4-oh-tempo
CHEBI:180664
4-hydroxy-2,2,6,6-tetramethylpiperidinyloxyl
piperidinooxy, 4-hydroxy-2,2,6,6-tetramethyl-
1-piperidinyloxy, 4-hydroxy-2,2,6,6-tetramethyl-
4-hydroxy-2,2,6,6-tetramethylpiperidinooxyl
hytempo
2,2,6,6-tetramethyl-4-hydroxypiperidinooxy
einecs 218-760-9
4-oxypiperidol
2,2,6,6-tetramethyl-4-hydroxypiperidine 1-oxide
nsc 142784
4-hydroxy-2,2,6,6-tetramethylpiperidin-1-oxyl
2,2,6,6-tetramethyl-4-hydroxypiperidinooxy radical
ccris 4555
2,2,6,6-tetramethyl-4-piperidinol-n-oxyl
nr 1
nsc-142784
4-hydroxy-tempo, free radical
4-hydroxy-tempo, 97%
4-hydroxy-2,2,6,6-tetramethylpiperidine-1-oxyl
4-hydroxy-2,2,6,6-tetramethyl-piperidinooxy
H0865
spj-701
CHEMBL607023
zj-701
mbm-02
NCGC00248196-01
4-hydroxy-2,2,6,6-tetramethyl piperidinyloxy
hsdb 8014
u78zx2f65x ,
1-piperidinyloxy, 4-hydroxy-2,2,6,6-tetramethyl
ec 218-760-9
unii-u78zx2f65x
NCGC00254776-01
dtxcid2021280
4-hydroxy-2,2,6,6-tetramethylpiperidin-1-yl)oxidanyl
dtxsid4041280 ,
tox21_300872
cas-2226-96-2
piperidinoxy,4-hydroxy-2,2,6,6-tetramethyl, sebacate
4-hydroxy-2,2,6,6-tetramethyl piperidinyloxy free radical
FT-0618621
NCGC00248196-02
AKOS015908135
1-piperidinyloxy,4-hydroxy-2,2,6,6-tetramethyl-
4-hydroxy-2,2,6,6-tetramethylpiperidinlyoxy
tempol [who-dd]
4-hydroxy-2,2,6,6-tetramethylpiperidiney-1-oxyl
4-hydroxy-2,2,6,6-tetramethyl-piperidin-1-oxyl
tempol [mi]
2,2,6,6-tetramethyl-4-hydroxypiperidine 1-oxide radical
S2910
2,2,6,6-tetramethyl-4-hydroxy-1-piperidinyloxy radical
4-hydroxy tempo, free radical
4-hydroxy-tempo, purum, >=97.0% (chn)
CS-6034
HY-100561
DB12449
4-hydroxy-2,2,6,6-tetramethylpiperidine 1-oxyl free radical
AS-12539
HMS3884N22
CCG-266372
4-hydroxytempo

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (8)

RoleDescription
radical scavengerA role played by a substance that can react readily with, and thereby eliminate, radicals.
catalystA substance that increases the rate of a reaction without modifying the overall standard Gibbs energy change in the reaction.
nephroprotective agentAny protective agent that is able to prevent damage to the kidney.
anti-inflammatory agentAny compound that has anti-inflammatory effects.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
hepatoprotective agentAny compound that is able to prevent damage to the liver.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
aminoxylsRadicals derived from hydroxylamines by removal of the hydrogen atom from the hydroxy group. The synonymous terms nitroxyl radicals and nitroxides erroneously suggest the presence of a nitro group.
hydroxypiperidine
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency0.37220.001310.157742.8575AID1259256
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency43.18960.003041.611522,387.1992AID1159552; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency12.29980.000817.505159.3239AID1159527
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID705880Antiischemic activity against Wistar rat ischemic-reperfusion model assessed as wet/dry edema tissue ratio at 20 mg/kg, ip administered 15 minutes prior to induction of ischemia followed by administered 1 hr post reperfusion2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Novel TEMPO-PEG-RGDs conjugates remediate tissue damage induced by acute limb ischemia/reperfusion.
AID705879Antioxidant activity in rat thoracic aortic strips assessed as free radical scavenging activity by measuring reversal of acetylcholine-induced relaxation2012Journal of medicinal chemistry, May-10, Volume: 55, Issue:9
Novel TEMPO-PEG-RGDs conjugates remediate tissue damage induced by acute limb ischemia/reperfusion.
AID216890Mean surviving fraction of V79 cells following a 1-h exposure to H2O2.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Studies of structure-activity relationship of nitroxide free radicals and their precursors as modifiers against oxidative damage.
AID590087Antioxidant activity assessed as hydroxyl radical scavenging activity at 0.2 to 10 uM2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Synthesis and study of 2-amino-7-bromofluorenes modified with nitroxides and their precursors as dual anti-amyloid and antioxidant active compounds.
AID1679303Inhibition of NOX (unknown origin) assessed as reduction in peroxide production2018Bioorganic & medicinal chemistry letters, 01-15, Volume: 28, Issue:2
Discovery of 1-(4-((3-(4-methylpiperazin-1-yl)propyl)amino)benzyl)-5-(trifluoromethyl)pyridin-2(1H)-one, an orally active multi-target agent for the treatment of diabetic nephropathy.
AID1908169Induction of oxidative stress in HUVEC cells assessed as increase in intracellular ROS level at 5 uM incubated for 24 hrs by DCHF staining based inverted microscopic analysis2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis and biological evaluation of novel nitric oxide donors with antioxidative activity.
AID1474666Protection against ischemia/reperfusion-induced Wistar rat intestinal injury model assessed as effect on TNFalpha levels at 30 mg/kg administered as bolus dose pretreated for 5 mins followed by 12 hrs reperfusion and subsequent compound addition at 10 mg/2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Indole-TEMPO conjugates alleviate ischemia-reperfusion injury via attenuation of oxidative stress and preservation of mitochondrial function.
AID1353339Inhibition of COX2-induced PGE2 production in human A549 cells assessed as PGE2 level at 90 uM by ELISA (Rvb = 126 +/- 17 pg/ml)2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID1353351Growth inhibition of human NCI-H1299 cells assessed as cell growth at 90 uM in presence of aspirin by MTT assay relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID1166921Protection against H2O2-induced human HL60 cells assessed as reduction in DNA damage at 50 uM after 30 mins by comet assay2014Bioorganic & medicinal chemistry letters, Nov-01, Volume: 24, Issue:21
Two new antioxidant actinosporin analogues from the calcium alginate beads culture of sponge-associated Actinokineospora sp. strain EG49.
AID418552Antiradical activity against 2,2'-azobis-amidinopropane-induced linoleic acid peroxidation assessed as ratio of total oxyradical scavenging capacity to Trolox C2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Antioxidant and antiradical activities of resorcinarene tetranitroxides.
AID216900Mean surviving fraction of V79 cells following a 12-Gy dose of radiation.1998Journal of medicinal chemistry, Aug-27, Volume: 41, Issue:18
Studies of structure-activity relationship of nitroxide free radicals and their precursors as modifiers against oxidative damage.
AID590085Antioxidant activity assessed as peroxyl radical scavenging activity at 10 uM by fluorescence quenching assay2011European journal of medicinal chemistry, Apr, Volume: 46, Issue:4
Synthesis and study of 2-amino-7-bromofluorenes modified with nitroxides and their precursors as dual anti-amyloid and antioxidant active compounds.
AID1353341Anti-oxidant activity in human A549 cells assessed as inhibition of H2O2-induced ROS production by measuring ROS level at 100 uM by DCFH-DA staining based fluorescence assay (Rvb = 194 +/- 13%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1278457Increase in number of mouse 661W cells at 10 to 50 uM after 24 hrs by MTT assay relative to vehicle control2016Bioorganic & medicinal chemistry letters, Mar-01, Volume: 26, Issue:5
Design and synthesis of novel hybrid sydnonimine and prodrug useful for glaucomatous optic neuropathy.
AID1908168Effect on intracellular NO production in HUVEC cells assessed as increase in NO level at 5 uM incubated for 24 hrs by inverted microscopic analysis2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis and biological evaluation of novel nitric oxide donors with antioxidative activity.
AID1908171Cytoprotective activity against TBHP induced oxidative stress in human HUVEC cells assessed as increase in cell viability at 5 uM by CCK8 assay2022European journal of medicinal chemistry, Jun-05, Volume: 236Design, synthesis and biological evaluation of novel nitric oxide donors with antioxidative activity.
AID572090Antimalarial activity against Plasmodium falciparum NF54 by [3H]hypoxanthine incorporation assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1353346Growth inhibition of human NCI-H1299 cells assessed as cell growth at 90 uM by MTT assay relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID1474665Protection against ischemia/reperfusion-induced Wistar rat intestinal injury model assessed as reduction in lipid peroxidation by measuring lipid peroxide levels at 30 mg/kg administered as bolus dose pretreated for 5 mins followed by 12 hrs reperfusion a2017Bioorganic & medicinal chemistry, 05-01, Volume: 25, Issue:9
Indole-TEMPO conjugates alleviate ischemia-reperfusion injury via attenuation of oxidative stress and preservation of mitochondrial function.
AID1353353Growth inhibition of human NCI-H1299 cells assessed as cell growth at 900 uM in presence of aspirin by MTT assay relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID1353347Growth inhibition of human NCI-H1299 cells assessed as cell growth at 900 uM by MTT assay relative to control2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID572091Antimalarial activity against Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals.
AID1353343Effect on basal ROS level in human A549 cells at 100 uM by DCFH-DA staining based fluorescence assay (Rvb = 100 +/- 5%)2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
AID418551Antioxidant activity assessed as [drug]/[DPPH]causing 50% DPPH radical scavenging activity after 5 mins2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Antioxidant and antiradical activities of resorcinarene tetranitroxides.
AID1353337Inhibition of COX2-induced PGE2 production in human A549 cells assessed as PGE2 level at 90 uM in presence of aspirin by ELISA (Rvb = 126 +/- 17 pg/ml)2018European journal of medicinal chemistry, Mar-10, Volume: 147Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (5.26)18.2507
2000's1 (5.26)29.6817
2010's11 (57.89)24.3611
2020's6 (31.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 56.81

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index56.81 (24.57)
Research Supply Index3.00 (2.92)
Research Growth Index5.47 (4.65)
Search Engine Demand Index85.46 (26.88)
Search Engine Supply Index1.96 (0.95)

This Compound (56.81)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other19 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (9)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
The Effect of Antioxidants on Skin Blood Flow During Local Heating [NCT03680638]Phase 144 participants (Actual)Interventional2016-09-07Completed
The Effect of Local Antioxidant Therapy on Racial Differences in Vasoconstriction [NCT03680404]Phase 124 participants (Actual)Interventional2018-10-01Completed
Phase II Double-Blind, Placebo-Controlled Study of the Safety and Preliminary Effectiveness of MTS-01 for the Prevention of Alopecia Induced by Whole Brain Radiotherapy [NCT00801086]Phase 216 participants (Anticipated)Interventional2008-11-30Recruiting
[NCT05491928]0 participants Expanded AccessAvailable
A Pilot Trial Assessing the Feasibility of Delivering Topical MTS-01 to Reduce Dermatitis in Patients Receiving Intensity Modulated Radiation With Concurrent 5-Fluorouracil and Mitomycin-C for Stage I-III Carcinoma of the Anal Canal [NCT01324141]Phase 16 participants (Actual)Interventional2011-03-18Terminated(stopped due to Slow, insufficient accrual and failure to meet endpoints.)
A Phase 2/3, Adaptive, Randomized, Double-Blind, Placebo-Controlled Study to Examine the Effects of Tempol (MBM-02) in Subjects With COVID-19 Infection [NCT04729595]Phase 2/Phase 3248 participants (Actual)Interventional2021-09-01Terminated(stopped due to Study did not demonstrate statistical significance of its primary endpoint of clinical resolution of COVID-19 symptoms at day 14 versus placebo)
A Double Blind, Placebo Controlled Dose Range Finding Study to Assess the Safety, Pharmacokinetics, and Efficacy of Tempol for the Reduction of Severe Mucositis in Head and Neck Cancer Patients Undergoing Combined Radio- and Chemotherapy [NCT03480971]Phase 2120 participants (Anticipated)Interventional2019-05-13Recruiting
A Single Patient Compassionate Use of MBM-02 (Tempol) for the Treatment of Prostate Cancer [NCT04337099]0 participants Expanded AccessAvailable
An Open Label Study to Assess the Safety and Efficacy of MBM-01 for the Treatment of Ataxia Telangiectasia [NCT04887311]Phase 220 participants (Anticipated)Interventional2021-07-31Not yet recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01324141 (19) [back to overview]Duration of Overall Response (DOR)
NCT01324141 (19) [back to overview]Number of Participants That Required a Treatment Break Relative to Hematologic Toxicity (Non-dermatologic)
NCT01324141 (19) [back to overview]Number of Participants Treated With Topical MTS-01 and 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT) That Required Opiates
NCT01324141 (19) [back to overview]Number of Participants With 12 Month Disease Free Survival (DFS) Treated With 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT)
NCT01324141 (19) [back to overview]Number of Participants With 12-month Progression-free Survival Treated With 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT)
NCT01324141 (19) [back to overview]Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE)
NCT01324141 (19) [back to overview]Number of Participants With Tumor Tissue Negative for Human Papilloma Virus (HPV)
NCT01324141 (19) [back to overview]Overall Survival
NCT01324141 (19) [back to overview]Absolute Number of Cluster of Differentiation 3+ (CD3) Cells Per Gram of Biopsied Intestinal Tissue
NCT01324141 (19) [back to overview]Brief Pain Inventory Score
NCT01324141 (19) [back to overview]Mean Grade of Toxicity at Each Timepoint and Location for All Participants Who Underwent Treatment
NCT01324141 (19) [back to overview]Mean Percentage Pain Relief After Medication
NCT01324141 (19) [back to overview]Number of Cluster of Differentiation 4+ (CD4) Cells Per Gram of Biopsied Intestinal Tissue
NCT01324141 (19) [back to overview]Number of Cluster of Differentiation 8+ (CD8) Cells Per Gram of Biopsied Intestinal Tissue
NCT01324141 (19) [back to overview]Number of Grade 1 and Higher Adverse Events Possibly, Probably, or Definitely Related to Topical MTS-01 and 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT)
NCT01324141 (19) [back to overview]Pain Interference
NCT01324141 (19) [back to overview]Percentage of Total Viable Cells That Were Cluster of Differentiation 3+ (CD3+) Cells in Biopsied Tissue
NCT01324141 (19) [back to overview]Peripheral Blood Mononuclear Cells (Vascular Endothelial Growth Factor (VEGF), Tumor Necrosis Factor Alpha (TNF-alpha), Interleukin-7 (IL-7), and Transforming Growth Factor Beta-1 (TGF-beta1) Cell Counts at Baseline and Course 1 Day 28
NCT01324141 (19) [back to overview]Ratio of the Number of Cluster of Differentiation 4 (CD4): Cluster of Differentiation 8 (CD8) Cells in the Circulation and Tissue Pre and Post Treatment

Duration of Overall Response (DOR)

Duration of overall response is measured from the time measurement criteria are met for Complete Response until the first date that recurrent or progressive disease is objectively document. Complete Response was measured by the Response Evaluation Criteria in Solid Tumors (RECIST0 version 1.1. Complete Response is disappearance of all target lesions. (NCT01324141)
Timeframe: 12 months of follow up, approximately 14 months

Interventionmonths (Median)
1/Chemo + RadiationNA

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Number of Participants That Required a Treatment Break Relative to Hematologic Toxicity (Non-dermatologic)

Number of participants that required a treatment break relative to hematologic (e.g. thrombocytopenia, leukopenia) toxicity (non-dermatologic). (NCT01324141)
Timeframe: From beginning until completion of radiation treatment up to 46 days

InterventionParticipants (Count of Participants)
1/Chemo + Radiation0

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Number of Participants Treated With Topical MTS-01 and 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT) That Required Opiates

Opiates are strong drugs prescribed by prescription used for maximum pain relief. (NCT01324141)
Timeframe: Completion of study, approximately 14 months after start of treatment

InterventionParticipants (Count of Participants)
1/Chemo + Radiation5

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Number of Participants With 12 Month Disease Free Survival (DFS) Treated With 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT)

DFS is defined as the duration of time from start of treatment to time of progression. Progression was assessed by the Response Evaluation Criteria in Solid Tumors (RECIST0 version 1.1. Progression is at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study. And the appearance of one or more new lesions. (NCT01324141)
Timeframe: 12 months

InterventionParticipants (Count of Participants)
1/Chemo + Radiation4

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Number of Participants With 12-month Progression-free Survival Treated With 5-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT)

PFS is defined as the duration of time from start of treatment to time of progression or death, whichever occurs first. Progression was assessed by the Response Evaluation Criteria in Solid Tumors (RECIST0 version 1.1. Progression is at least a 20% increase in the sum of the diameters of target lesions, taking as reference the smallest sum on study. And the appearance of one or more new lesions. (NCT01324141)
Timeframe: 12 months

InterventionParticipants (Count of Participants)
1/Chemo + Radiation4

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Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE)

Here is the number of participants with serious and non-serious adverse events assessed by the Common Terminology Criteria for Adverse Events (CTCAE). A non-serious adverse event is any untoward medical occurrence. A serious adverse event is an adverse event or suspected adverse reaction that results in death, a life-threatening adverse drug experience, hospitalization, disruption of the ability to conduct normal life functions, congenital anomaly/birth defect or important medical events that jeopardize the patient or subject and may require medical or surgical intervention to prevent one of the previous outcomes mentioned. (NCT01324141)
Timeframe: Date treatment consent signed to date off study, approximately, 36 months and 10 days.

InterventionParticipants (Count of Participants)
1/Chemo + Radiation5

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Number of Participants With Tumor Tissue Negative for Human Papilloma Virus (HPV)

HPV is a sexually transmitted infection that can cause warts and cervical cancer. HPV test detects deoxyribonucleic acid (DNA) or ribonucleic acid (RNA) of HPV in a cell sample (i.e. cervical). (NCT01324141)
Timeframe: Pretreatment

InterventionParticipants (Count of Participants)
1/Chemo + Radiation5

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Overall Survival

OS is defined as the duration of time from start of treatment to time of death. (NCT01324141)
Timeframe: start of treatment to time of death, approximately 14 months

Interventionmonths (Median)
1/Chemo + RadiationNA

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Absolute Number of Cluster of Differentiation 3+ (CD3) Cells Per Gram of Biopsied Intestinal Tissue

Absolute number of Cluster of differentiation 3+ (CD3) cells per gram of biopsied intestinal tissue. The number of CD3 positive cells were analyzed with flow cytometry of cellular suspensions from biopsy tissue. (NCT01324141)
Timeframe: Baseline and 1 year follow up

InterventionCD3+cells/gm tissue(x 10^5) (Mean)
Baseline1 year follow up
1/Chemo + Radiation22.9813.62

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Brief Pain Inventory Score

The Brief Pain Inventory Scale is a questionnaire that asks the participant to rate their pain on a scale of 0 (no pain) to 10 (worst pain). (NCT01324141)
Timeframe: Baseline, Week 3, Week 6, 1 month follow up, and 3 months follow up

InterventionScores on a scale (Mean)
Worst pain at baselineWorst pain at treatment week 3Worst pain at treatment week 6Worst pain at 1 month follow upWorst pain at 3 months follow upLeast pain at baselineLeast pain at treatment week 3least pain at treatment week 6Least pain at 1 month follow upLeast pain at 3 months follow upAverage pain at baselineAverage pain at treatment week 3Average pain at treatment week 6Average pain at 1 month follow upAverage pain at 3 months follow upPain at time of survey at baselinePain at time of survey at treatment week 3Pain at time of survey at treatment week 6Pain at time of survey a 1 month follow upPain at time of survey at 3 months follow up
1/Chemo + Radiation4.83.57.23.12.11.41.53.61.22.81.81.95.02.03.01.61.35.42.22.2

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Mean Grade of Toxicity at Each Timepoint and Location for All Participants Who Underwent Treatment

RTOG grade 1-5 were used to assess skin toxicity in the groin (right and left inguinal area) and gluteal cleft, as well as two control sites. Grade 0 is no skin toxicity, Grade 1 is follicular, faint or dull erythema, Grade 3 is tender or bright erythema, Grade 3 is confluent, moist desquamation, Grade 4 is ulceration, hemorrhage, or necrosis, and Grade 5 is death due to radiation toxicity. (NCT01324141)
Timeframe: baseline, weeks 1-6, follow up at 1 week, follow up at 2 weeks, and follow up at 4 weeks

,,,,
InterventionGrade (Mean)
BaselineWeek 1Week 2Week 3Week 4Week 5Week 6Follow up at 1 weekFollow up at 2 weeksFollow up at 4 weeks
Gluteal Cleft0000.40.611.21.81.20.4
Left Inguinal Area0000.20.60.81.2110.2
Left Inguinal Control (C1)0000.20.20.20.40.60.80.6
Right Inguinal Area0000.20.60.81.2110.2
Umbilical Control (C2)0000000000

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Mean Percentage Pain Relief After Medication

The Brief Pain Inventory Scale questionnaire were used to assess pain relief after medication. Participants rated pain relief on a scale of 0% (no relief) to 100% (complete relief) and a mean and full range were reported. (NCT01324141)
Timeframe: Baseline, Week 3, Week 6, 1 month follow up, and 3 months follow up

Interventionpercentage pain relief (Mean)
BaselineTreatment week 3Treatment week 61 month follow up3 months follow up
1/Chemo + Radiation90.093.844.089.083.0

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Number of Cluster of Differentiation 4+ (CD4) Cells Per Gram of Biopsied Intestinal Tissue

Number of Cluster of Differentiation 4+ (CD4) cells per gram of biopsied intestinal tissue. The number of CD4 positive cells were analyzed with flow cytometry of cellular suspensions from biopsy tissue. (NCT01324141)
Timeframe: Baseline and 1 year follow up

InterventionCD4+cells/gm tissue(x 10^5) (Mean)
Baseline1 year follow up
1/Chemo + Radiation17.6412.72

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Number of Cluster of Differentiation 8+ (CD8) Cells Per Gram of Biopsied Intestinal Tissue

Number of Cluster of differentiation 8+ (CD8) cells per gram of biopsied intestinal tissue. The number of CD8 positive cells were analyzed with flow cytometry of cellular suspensions from biopsy tissue. (NCT01324141)
Timeframe: Baseline and 1 year follow up

InterventionCD8+cells/gm tissue(x 10^5) (Mean)
Baseline1 year follow up
1/Chemo + Radiation4.84.0

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Pain Interference

The Brief Pain Inventory Scale questionnaire were used to assess pain interference. Participants rated pain interference on a scale of 0 (does not interfere) to 10 (completely interferes). (NCT01324141)
Timeframe: Baseline, Week 3, Week 6, 1 month follow up, and 3 months follow up

InterventionScores on a scale (Mean)
Pain interference at baselinePain interference at treatment week 3Pain interference at treatment week 6Pain interference at 1 month follow upPain interference at 3 months follow up
1/Chemo + Radiation1.733.006.703.171.87

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Percentage of Total Viable Cells That Were Cluster of Differentiation 3+ (CD3+) Cells in Biopsied Tissue

Percentage of total viable cells that were Cluster of differentiation 3+ (CD3+) cells in biopsied tissue. (NCT01324141)
Timeframe: Baseline and 1 year

Interventionpercentage of cells (Mean)
Baseline1 year
1/Chemo + Radiation7.934.40

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Peripheral Blood Mononuclear Cells (Vascular Endothelial Growth Factor (VEGF), Tumor Necrosis Factor Alpha (TNF-alpha), Interleukin-7 (IL-7), and Transforming Growth Factor Beta-1 (TGF-beta1) Cell Counts at Baseline and Course 1 Day 28

Peripheral blood mononuclear cells (Vascular Endothelial Growth Factor (VEGF), Tumor Necrosis Factor alpha (TNF-alpha), Interleukin-7 (IL-7), and Transforming Growth Factor beta-1 (TGF-beta1) were sampled from peripheral blood from rectal associated lymphoid tissue to evaluate immune cell subsets at baseline and after treatment with MTS-0 and 15-Fluoruracil (5-FU)/Mitomycin C (MMC)/Intensity-modulated Radiotherapy (IMRT). It is unknown if a lower or higher numbers has prognostic significance. (NCT01324141)
Timeframe: Baseline and Course 1 Day 28

Interventionpg/ml (Mean)
VEGF at baselineVEGF at Course 1 Day 28TNF-alpha at baselineTNF-alpha at Course 1 Day 28IL-7 at baselineIL-7 at Course 1 Day 28TGF-beta 1 at baselineTGF-beta 1 at Course 1 Day 28
1/Chemo + Radiation151.24127.263.363.2111.3215.62144357946

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Ratio of the Number of Cluster of Differentiation 4 (CD4): Cluster of Differentiation 8 (CD8) Cells in the Circulation and Tissue Pre and Post Treatment

Ratio of the number Cluster of Differentiation 4 (CD4): Cluster of Differentiation 8 (CD8) cells in the circulation and tissue pre and post treatment. The number of cells of CD4 are divided by the number of cells of CD8. (NCT01324141)
Timeframe: Pre-treatment and post treatment tissue (CD4), and pre-treatment and post treatment circulation (CD8)

InterventionRatio of CD4:CD8 cells (Mean)
CD4:CD8 Pre-treatment tissueCD4:CD8 post treatment tissueCD4:CD8 pre-treatment circulationCD4:CD8 post treatment circulation
1/Chemo + Radiation5.21.892.951.56

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