Compounds > gc 1 compound
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gc 1 compound

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Description

GC 1 compound: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9862248
CHEMBL ID107400
CHEBI ID79988
SCHEMBL ID282119
MeSH IDM0369827

Synonyms (44)

Synonym
gtpl2639
2-[4-[(4-hydroxy-3-propan-2-ylphenyl)methyl]-3,5-dimethylphenoxy]acetic acid
211110-63-3
gc-1
sobetirome
gc 1 compound
DB07425
[4-(4-hydroxy-3-isopropyl-benzyl)-3,5-dimethyl-phenoxy]-acetic acid(gc-1)
3,5-dimethyl-4-(4''-hydroxy-3''-isopropylbenzyl)phenoxyacetic acid
bdbm50115668
[4-(4-hydroxy-3-isopropyl-benzyl)-3,5-dimethyl-phenoxy]-acetic acid
{4-[4-hydroxy-3-(1-methylethyl)benzyl]-3,5-dimethylphenoxy}acetic acid
B72 ,
CHEMBL107400 ,
chebi:79988 ,
sobetirome (usan)
D09381
qrx 431
qrx-431
xq31741e9q ,
unii-xq31741e9q
sobetirome [usan:inn]
gc 1
HY-14823
3IMY
CS-0956
(4-{[4-hydroxy-3-(1-methylethyl)phenyl]methyl}-3,5-dimethylphenoxy)acetic acid
sobetirome [inn]
sobetirome [usan]
sobetirome [who-dd]
SCHEMBL282119
2-[4-[[4-hydroxy-3-(1-methylethyl)phenyl]methyl]-3,5-dimethylphenoxy]acetic acid
AKOS024458221
2-(4-(4-hydroxy-3-isopropylbenzyl)-3,5-dimethylphenoxy)acetic acid
BCP23779
gc-1; gc1; gc 1; qrx-431; qrx 431; qrx431
DTXSID60891557
FT-0735243
Q27088838
A905652
F84869
BS-42167
acetic acid, 2-[4-[[4-hydroxy-3-(1-methylethyl)phenyl]methyl]-3,5-dimethylphenoxy]-
gc-1;qrx-431

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" In vivo pharmacokinetic evaluation showed effective GC-1 plasma concentrations, which resulted in significant reductions in body weight after just one week of treatment when compared to the NMD releasing vehicle only (PBS)."( A pharmacokinetic study of GC-1 delivery using a nanochannel membrane device.
Ballerini, A; Chua, CYX; Filgueira, CS; Gilbert, AL; Grattoni, A; Jain, P; Nicolov, E; Scaglione, F; Smith, ZW, 2017)		0.46

Bioavailability

ExcerptReferenceRelevance
" Because of the low oral bioavailability of PA 22c, a series of prodrugs was synthesized and screened for oral efficacy in the CFR assay."( Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
Boyer, SH; Cable, EE; Erion, MD; Fujitaki, JM; Godwin, JL; Hecker, SJ; Hou, J; Jacintho, JD; Jiang, H; Li, H; Li, W; Reddy, MV; Schulz, WG; Wu, R, 2008)		0.35

Dosage Studied

ExcerptRelevanceReference
" Additional dose-response studies in hypercholesteremic rats confirmed the preferential effect of GC-1 on TRbeta-mediated parameters by showing a much higher potency to influence cholesterol and TSH than heart rate."( The thyroid hormone receptor-beta-selective agonist GC-1 differentially affects plasma lipids and cardiac activity.
Baxter, JD; Chiellini, G; Dillmann, WH; Gloss, B; Grover, GJ; Scanlan, TS; Swanson, E; Trost, SU; Volodarsky, T; Wang-Iverson, DB; Zhang, H, 2000)		0.31
" The most potent natural thyroid hormone, 3,5,3'-triidothyronine or T3, shows similar binding affinity and transactivation dose-response curves for both thyroid hormone receptor isotypes, designated TRalpha and TRbeta."( Induction of larval tissue resorption in Xenopus laevis tadpoles by the thyroid hormone receptor agonist GC-1.
Chiellini, G; Ermio, DJ; Furlow, JD; Hsu, M; Lim, W; Scanlan, TS; Yang, HY, 2004)		0.32
" Instead, the effects of TR activation on glycemia varied widely and were found to depend upon the time of treatment as well as the compound and dosage used."( The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivity in ob/ob mice.
Cimini, SL; Lin, JZ; Martagón, AJ; Phillips, KJ; Webb, P, 2015)		0.42
" Dosing male C57BL/6 mice with sobetirome and Sob-AM2 at concentrations ≥10 μg/kg/d for 29 days induces a state similar to central hypothyroidism characterized by depleted circulating T4 and T3 and normal TSH levels."( Hypothalamic-Pituitary-Thyroid Axis Perturbations in Male Mice by CNS-Penetrating Thyromimetics.
Bourdette, D; Ferrara, SJ; Scanlan, TS, 2018)		0.48
" Treatment with GC-1 upregulated the transcription of CPT1A in the human hepatocyte-derived Huh-7 cell line with a dose-response comparable to that of the native THR ligand, triiodothyronine (T3)."( Regulation of gene transcription by thyroid hormone receptor β agonists in clinical development for the treatment of non-alcoholic steatohepatitis (NASH).
Beigelman, LN; Blatt, LM; Chanda, S; Deval, J; Gupta, K; Jekle, A; Lin, TI; Luong, XG; McGowan, D; Misner, D; Mukherjee, S; Raboisson, P; Stevens, SK; Stoycheva, A; Symons, JA; Vandyck, K; Williams, C, 2020)		0.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
diarylmethaneAny compound containing two aryl groups connected by a single C atom.
[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 (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thyroid hormone receptor alphaHomo sapiens (human)Ki0.00110.00020.00390.0096AID345695
Thyroid hormone receptor betaHomo sapiens (human)Ki0.00030.00010.00070.0023AID345696
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thyroid hormone receptor alphaHomo sapiens (human)EC50 (µMol)0.02400.00040.25843.7400AID1139981; AID213169
Thyroid hormone receptor alphaHomo sapiens (human)Kd0.00110.00010.00210.0098AID1799448; AID213172; AID213173; AID715451
Thyroid hormone receptor betaHomo sapiens (human)EC50 (µMol)0.01250.00020.03480.2400AID1139979; AID213180
Thyroid hormone receptor betaHomo sapiens (human)Kd0.00020.00010.00170.0098AID1799448; AID213183; AID213185; AID715452
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (33)

Processvia Protein(s)Taxonomy
cartilage condensationThyroid hormone receptor alphaHomo sapiens (human)
ossificationThyroid hormone receptor alphaHomo sapiens (human)
regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
learning or memoryThyroid hormone receptor alphaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor alphaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor alphaHomo sapiens (human)
response to coldThyroid hormone receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of RNA polymerase II transcription preinitiation complex assemblyThyroid hormone receptor alphaHomo sapiens (human)
erythrocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid gland developmentThyroid hormone receptor alphaHomo sapiens (human)
regulation of myeloid cell apoptotic processThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcriptionThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of female receptivityThyroid hormone receptor alphaHomo sapiens (human)
regulation of lipid catabolic processThyroid hormone receptor alphaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of cold-induced thermogenesisThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of DNA-templated transcription initiationThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
cell differentiationThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor alphaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor alphaHomo sapiens (human)
positive regulation of thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
DNA-templated transcriptionThyroid hormone receptor betaHomo sapiens (human)
sensory perception of soundThyroid hormone receptor betaHomo sapiens (human)
negative regulation of female receptivityThyroid hormone receptor betaHomo sapiens (human)
regulation of heart contractionThyroid hormone receptor betaHomo sapiens (human)
female courtship behaviorThyroid hormone receptor betaHomo sapiens (human)
mRNA transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell developmentThyroid hormone receptor betaHomo sapiens (human)
type I pneumocyte differentiationThyroid hormone receptor betaHomo sapiens (human)
cellular response to thyroid hormone stimulusThyroid hormone receptor betaHomo sapiens (human)
retinal cone cell apoptotic processThyroid hormone receptor betaHomo sapiens (human)
retinoic acid receptor signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
cell differentiationThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone mediated signaling pathwayThyroid hormone receptor betaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIThyroid hormone receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (16)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor alphaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor alphaHomo sapiens (human)
protein bindingThyroid hormone receptor alphaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor alphaHomo sapiens (human)
TBP-class protein bindingThyroid hormone receptor alphaHomo sapiens (human)
protein domain specific bindingThyroid hormone receptor alphaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor alphaHomo sapiens (human)
general transcription initiation factor bindingThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificThyroid hormone receptor betaHomo sapiens (human)
transcription coactivator bindingThyroid hormone receptor betaHomo sapiens (human)
DNA bindingThyroid hormone receptor betaHomo sapiens (human)
DNA-binding transcription factor activityThyroid hormone receptor betaHomo sapiens (human)
nuclear receptor activityThyroid hormone receptor betaHomo sapiens (human)
protein bindingThyroid hormone receptor betaHomo sapiens (human)
zinc ion bindingThyroid hormone receptor betaHomo sapiens (human)
enzyme bindingThyroid hormone receptor betaHomo sapiens (human)
chromatin DNA bindingThyroid hormone receptor betaHomo sapiens (human)
thyroid hormone bindingThyroid hormone receptor betaHomo sapiens (human)
sequence-specific double-stranded DNA bindingThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingThyroid hormone receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleusThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor alphaHomo sapiens (human)
cytosolThyroid hormone receptor alphaHomo sapiens (human)
chromatinThyroid hormone receptor alphaHomo sapiens (human)
nucleusThyroid hormone receptor alphaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor alphaHomo sapiens (human)
nucleoplasmThyroid hormone receptor betaHomo sapiens (human)
nuclear bodyThyroid hormone receptor betaHomo sapiens (human)
RNA polymerase II transcription regulator complexThyroid hormone receptor betaHomo sapiens (human)
chromatinThyroid hormone receptor betaHomo sapiens (human)
nucleusThyroid hormone receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (55)

Assay IDTitleYearJournalArticle
AID1799448TR Receptor Ligand Binding Assay from Article 10.1016/s1074-5521(98)90168-5: \\A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.\\1998Chemistry & biology, Jun, Volume: 5, Issue:6
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
AID345698Agonist activity at thyroid hormone receptor in Sprague-Dawley rat assessed as heart mGPDH activity at 1 mg/kg administered through osmotic pump infusion per ug protein2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
AID1073538Selectivity ratio of IC50 for human recombinant TRalpha1 ligand binding domain to IC50 for human recombinant TRbeta1 ligand binding domain2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists.
AID213183Binding affinity against human Thyroid hormone receptor beta 1 (hTRbeta1) using radiolabeled T32002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID213180Half-maximum activation of human Thyroid hormone receptor beta 1 (hTRbeta1)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID1139979Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID1515608Brain to serum permeability coefficient, Kp of the compound in C57BL/6 mouse at 3.05 umol/kg, ip after 1 hr by LC-MS/MS analysis2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Structure-Activity Relationships of Central Nervous System Penetration by Fatty Acid Amide Hydrolase (FAAH)-Targeted Thyromimetic Prodrugs.
AID1139989Toxicity in thyroidectomized rat assessed as T3 activity at 3 ug, ip measured after 6 hrs2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID1364742Oral bioavailability in C57Bl/6 mouse at 3.05 umol/kg administered via oral gavage by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID213185Binding affinity of compound was determined against thyroid hormone receptor beta 12003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Structural determinants of selective thyromimetics.
AID1364744Upregulation of Hr expression levels in ip dosed mouse brain for 7 days measured after 2 hrs post last dose by STBR green dye-based qPCR analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1364743Clearance in C57Bl/6 mouse at 3.05 umol/kg, iv by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1713815Ratio of AUC in C57Bl/6 mouse brain to serum at 1.5 microM/Kg, ip upto 8 hrs by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID213172Binding affinity against human Thyroid hormone receptor alpha-1 (hTRalpha1) using radiolabeled T32002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID1364733Ratio of drug level in C57Bl/6 mouse brain to serum at 1.5 umol/kg, ip after 1 hr by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1140054Selectivity ratio of EC50 for recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) to EC50 for recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) relative to T32014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID1515622Agonist activity at human TRbeta after 24 hrs by cell based luciferase reporter gene assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Structure-Activity Relationships of Central Nervous System Penetration by Fatty Acid Amide Hydrolase (FAAH)-Targeted Thyromimetic Prodrugs.
AID345695Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
AID1364741Elimination half life in C57Bl/6 mouse at 3.05 umol/kg, iv by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1713813AUC (0 to t) in C57Bl/6 mouse brain at 1.5 microM/Kg, ip upto 8 hrs by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID1713818Half life in iv dosed mouse2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID1364735AUC (0 to t) in C57Bl/6 mouse brain at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID715451Binding affinity to human TRalpha12012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.
AID715452Binding affinity to human TRbeta12012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.
AID345696Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
AID1713814AUC (0 to t) in C57Bl/6 mouse liver at 1.5 microM/Kg, ip upto 8 hrs by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID213177Activation of human Thyroid hormone receptor beta 1 (hTRbeta1)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID345697Agonist activity at thyroid hormone receptor in Sprague-Dawley rat assessed as liver mGPDH activity at 1 mg/kg administered through osmotic pump infusion per ug protein2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
AID1364738AUC (0 to t) in C57Bl/6 mouse heart at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID213169Half-maximum activation of human Thyroid hormone receptor alpha-1 (hTRalpha1)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID1364740Ratio of AUC (0 to t) in C57Bl/6 mouse brain to serum at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1877208Reduction in C26:0 LPC level in ABCD1 (-/y) knock out mouse brain at 0.4 to 2 mg/kg, ip administered daily measured after 4.5 months by LC-MS/MS analysis2021Journal of medicinal chemistry, 12-23, Volume: 64, Issue:24
Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1.
AID1364739AUC (0 to t) in C57Bl/6 mouse kidney at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1364736AUC (0 to t) in C57Bl/6 mouse serum at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1713812AUC (0 to t) in C57Bl/6 mouse serum at 1.5 microM/Kg, ip upto 8 hrs by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID345694Selectivity for human TRbeta1 over human TRalpha12008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
AID1364732Drug uptake in C57Bl/6 mouse brain at 1.5 umol/kg, ip after 1 hr by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID715453Antidyslipidemic activity in human assessed as reduction in LDL cholesterol at 100 ug administered QD relative to control2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.
AID1139980Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T32014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID213167Activation of human Thyroid hormone receptor alpha1 (hTRalpha1)2002Journal of medicinal chemistry, Jul-18, Volume: 45, Issue:15
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
AID1713811Prodrug conversion in C57Bl/6 mouse brain assessed as increase in sobetirome level at 1.5 micromol/kg, ip after 30 mins by LC-MS/MS analysis relative to sobetirome control2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID1713816Ratio of AUC in C57Bl/6 mouse brain to liver at 1.5 microM/Kg, ip upto 8 hrs by LC-MS/MS analysis2016Bioorganic & medicinal chemistry, 11-15, Volume: 24, Issue:22
Sobetirome prodrug esters with enhanced blood-brain barrier permeability.
AID234536Selectivity of compound was determined against thyroid hormone receptor2003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Structural determinants of selective thyromimetics.
AID1515621Agonist activity at human TRalpha after 24 hrs by cell based luciferase reporter gene assay2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Structure-Activity Relationships of Central Nervous System Penetration by Fatty Acid Amide Hydrolase (FAAH)-Targeted Thyromimetic Prodrugs.
AID1139981Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay2014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID1515607Drug uptake in C57BL/6 mouse serum at 3.05 umol/kg, ip after 1 hr by LC-MS/MS analysis2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Structure-Activity Relationships of Central Nervous System Penetration by Fatty Acid Amide Hydrolase (FAAH)-Targeted Thyromimetic Prodrugs.
AID1515606Drug uptake in C57BL/6 mouse brain at 3.05 umol/kg, ip after 1 hr by LC-MS/MS analysis2019ACS medicinal chemistry letters, Jan-10, Volume: 10, Issue:1
Structure-Activity Relationships of Central Nervous System Penetration by Fatty Acid Amide Hydrolase (FAAH)-Targeted Thyromimetic Prodrugs.
AID1073497Reduction in LDL-cholesterol in healthy human at 100 ug qd for 2 weeks2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists.
AID1139982Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay relative to T32014Journal of medicinal chemistry, May-22, Volume: 57, Issue:10
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dys
AID213173Binding affinity of compound was determined against Thyroid hormone receptor alpha12003Journal of medicinal chemistry, Jul-03, Volume: 46, Issue:14
Structural determinants of selective thyromimetics.
AID1364737AUC (0 to t) in C57Bl/6 mouse liver at 1.5 umol/kg, ip by LC-MS/MS analysis2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
AID1346773Human Thyroid hormone receptor-alpha (1A. Thyroid hormone receptors)1990Molecular endocrinology (Baltimore, Md.), Feb, Volume: 4, Issue:2
Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2
AID1346752Human Thyroid hormone receptor-beta (1A. Thyroid hormone receptors)1977Proceedings of the National Academy of Sciences of the United States of America, Aug, Volume: 74, Issue:8
Opiate-dependent modulation of adenylate cyclase.
AID1346752Human Thyroid hormone receptor-beta (1A. Thyroid hormone receptors)1998Chemistry & biology, Jun, Volume: 5, Issue:6
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (95)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.05)18.7374
1990's2 (2.11)18.2507
2000's31 (32.63)29.6817
2010's40 (42.11)24.3611
2020's21 (22.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.12

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.12 (24.57)
Research Supply Index4.58 (2.92)
Research Growth Index5.71 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews12 (12.37%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other85 (87.63%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
gamma-aminobutyric acid
gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4.		2.0310amino acid zwitterion;
gamma-amino acid;
monocarboxylic acid		human metabolite;
neurotransmitter;
Saccharomyces cerevisiae metabolite;
signalling molecule
methane
Methane: The simplest saturated hydrocarbon. It is a colorless, flammable gas, slightly soluble in water. It is one of the chief constituents of natural gas and is formed in the decomposition of organic matter. (Grant & Hackh's Chemical Dictionary, 5th ed). methane : A one-carbon compound in which the carbon is attached by single bonds to four hydrogen atoms. It is a colourless, odourless, non-toxic but flammable gas (b.p. -161degreeC).		2.3110alkane;
gas molecular entity;
mononuclear parent hydride;
one-carbon compound		bacterial metabolite;
fossil fuel;
greenhouse gas
ethanolamine
[no description available]		2.1510ethanolamines;
primary alcohol;
primary amine		Escherichia coli metabolite;
human metabolite;
mouse metabolite
glycine
[no description available]		2.0210alpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid		EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
nickel
Nickel: A trace element with the atomic symbol Ni, atomic number 28, and atomic weight 58.69. It is a cofactor of the enzyme UREASE.. nickel ion : A nickel atom having a net electric charge.. nickel atom : Chemical element (nickel group element atom) with atomic number 28.		2.6920metal allergen;
nickel group element atom		epitope;
micronutrient
phthalic acid
phthalic acid: RN given refers to parent cpd; structure in Merck Index, 9th ed, #7178. phthalic acid : A benzenedicarboxylic acid cosisting of two carboxy groups at ortho positions.		2.610benzenedicarboxylic acidhuman xenobiotic metabolite
uracil
2,4-dihydroxypyrimidine: a urinary biomarker for bipolar disorder		3.7620pyrimidine nucleobase;
pyrimidone		allergen;
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
prodrug;
Saccharomyces cerevisiae metabolite
iopanoic acid
Iopanoic Acid: Radiopaque medium used as diagnostic aid.		2.0210monocarboxylic acid
3,3',5-triiodothyroacetic acid
tiratricol : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)acetic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxy-3-iodophenoxy group. It is a thyroid hormone analogue that has been used in the treatment of thyroid hormone resistance syndrome.		4.0440
thyroxine
Thyroxine: The major hormone derived from the thyroid gland. Thyroxine is synthesized via the iodination of tyrosines (MONOIODOTYROSINE) and the coupling of iodotyrosines (DIIODOTYROSINE) in the THYROGLOBULIN. Thyroxine is released from thyroglobulin by proteolysis and secreted into the blood. Thyroxine is peripherally deiodinated to form TRIIODOTHYRONINE which exerts a broad spectrum of stimulatory effects on cell metabolism.. thyroxine : An iodothyronine compound having iodo substituents at the 3-, 3'-, 5- and 5'-positions.		5.441102-halophenol;
iodophenol;
L-phenylalanine derivative;
non-proteinogenic L-alpha-amino acid;
thyroxine zwitterion;
thyroxine		antithyroid drug;
human metabolite;
mouse metabolite;
thyroid hormone
triiodothyronine
Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3.. 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism.		8.434102-halophenol;
amino acid zwitterion;
iodophenol;
iodothyronine		human metabolite;
mouse metabolite;
thyroid hormone
glutamine
Glutamine: A non-essential amino acid present abundantly throughout the body and is involved in many metabolic processes. It is synthesized from GLUTAMIC ACID and AMMONIA. It is the principal carrier of NITROGEN in the body and is an important energy source for many cells.. L-glutamine : An optically active form of glutamine having L-configuration.. glutamine : An alpha-amino acid that consists of butyric acid bearing an amino substituent at position 2 and a carbamoyl substituent at position 4.		2.2110amino acid zwitterion;
glutamine family amino acid;
glutamine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		EC 1.14.13.39 (nitric oxide synthase) inhibitor;
Escherichia coli metabolite;
human metabolite;
metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
gliotoxin
Gliotoxin: A fungal toxin produced by various species of Trichoderma, Gladiocladium fimbriatum, Aspergillus fumigatus, and Penicillium. It is used as an immunosuppressive agent.. gliotoxin : A pyrazinoindole with a disulfide bridge spanning a dioxo-substituted pyrazine ring; mycotoxin produced by several species of fungi.		2.2110dipeptide;
organic disulfide;
organic heterotetracyclic compound;
pyrazinoindole		antifungal agent;
EC 2.5.1.58 (protein farnesyltransferase) inhibitor;
immunosuppressive agent;
mycotoxin;
proteasome inhibitor
asparagine
Asparagine: A non-essential amino acid that is involved in the metabolic control of cell functions in nerve and brain tissue. It is biosynthesized from ASPARTIC ACID and AMMONIA by asparagine synthetase. (From Concise Encyclopedia Biochemistry and Molecular Biology, 3rd ed). asparagine : An alpha-amino acid in which one of the hydrogens attached to the alpha-carbon of glycine is substituted by a 2-amino-2-oxoethyl group.		210amino acid zwitterion;
asparagine;
aspartate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
histidine
Histidine: An essential amino acid that is required for the production of HISTAMINE.. L-histidine : The L-enantiomer of the amino acid histidine.. histidine : An alpha-amino acid that is propanoic acid bearing an amino substituent at position 2 and a 1H-imidazol-4-yl group at position 3.		2.0210amino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
arginine
Arginine: An essential amino acid that is physiologically active in the L-form.. arginine : An alpha-amino acid that is glycine in which the alpha-is substituted by a 3-guanidinopropyl group.		2.0210arginine;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid		biomarker;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical
diphenyl
diphenyl: RN given refers to unlabeled cpd; structure		2.3110aromatic fungicide;
benzenes;
biphenyls		antifungal agrochemical;
antimicrobial food preservative
diethylhexyl phthalate
Diethylhexyl Phthalate: An ester of phthalic acid. It appears as a light-colored, odorless liquid and is used as a plasticizer for many resins and elastomers.. bis(2-ethylhexyl) phthalate : A phthalate ester that is the bis(2-ethylhexyl) ester of benzene-1,2-dicarboxylic acid.		2.610diester;
phthalate ester		androstane receptor agonist;
apoptosis inhibitor;
plasticiser
diiodotyrosine
Diiodotyrosine: A product from the iodination of MONOIODOTYROSINE. In the biosynthesis of thyroid hormones, diiodotyrosine residues are coupled with other monoiodotyrosine or diiodotyrosine residues to form T4 or T3 thyroid hormones (THYROXINE and TRIIODOTHYRONINE).. diiodotyrosine : A dihalogenated L-tyrosine which has two iodo-substituents on the benzyl moiety.. 3,5-diiodo-L-tyrosine : A diiodotyrosine that is L-tyrosine carrying iodo-substituents at positions C-3 and C-5 of the benzyl group. It is an intermediate in the thyroid hormone synthesis.		3.1810diiodotyrosine;
L-tyrosine derivative;
non-proteinogenic L-alpha-amino acid		human metabolite;
mouse metabolite
perfluorooctane
perfluorooctane: used in the treatment of giant retinal tears with proliferative vitreoretinopathy		2.2510fluoroalkane;
fluorocarbon
perfluorooctanoic acid
perfluorooctanoic acid: RN given refers to parent cpd. perfluorooctanoic acid : A fluoroalkanoic acid that is perfluorinated octanoic acid.		2.2510fluoroalkanoic acidcarcinogenic agent;
endocrine disruptor;
environmental contaminant;
surfactant;
xenobiotic
hydantoins
Hydantoins: Compounds based on imidazolidine dione. Some derivatives are ANTICONVULSANTS.. imidazolidine-2,4-dione : An imidazolidinone with oxo groups at position 2 and 4.		2.4620imidazolidine-2,4-dione
deoxyuridine
[no description available]		2.4110pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
thioflavin t
thioflavin T: RN given refers to chloride; structure. thioflavine T : An organic chloride salt having 2-[4-(dimethylamino)phenyl]-3,6-dimethyl-1,3-benzothiazol-3-ium as the counterion. It is widely used to visualise and quantify the presence of amyloids, both in vitro and in vivo.		2.3110organic chloride saltfluorochrome;
geroprotector;
histological dye
mono-(2-ethylhexyl)phthalate
mono-(2-ethylhexyl)phthalate: RN given refers to parent cpd. mono(2-ethylhexyl) phthalate : The mono(2-ethylhexyl) ester of benzene-1,2-dicarboxylic acid.		2.610phthalic acid monoester
3,3',5'-triiodothyronine
[no description available]		1.9710iodothyroninehuman metabolite
clemastine
Clemastine: A histamine H1 antagonist used as the hydrogen fumarate in hay fever, rhinitis, allergic skin conditions, and pruritus. It causes drowsiness.. clemastine : 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative properties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.		2.610monochlorobenzenes;
N-alkylpyrrolidine		anti-allergic agent;
antipruritic drug;
H1-receptor antagonist;
muscarinic antagonist
phenyl acetate
phenyl acetate: The ester formed between phenol and acetic acid. Don't confuse with phenylacetic acid derivatives listed under PHENYLACETATES.. phenyl acetate : An acetate ester obtained by the formal condensation of phenol with acetic acid.		10.4780benzenes;
phenyl acetates
tetraiodothyroacetic acid
tetraiodothyroacetic acid: RN given refers to parent cpd; structure. 3,3',5,5'-tetraiodothyroacetic acid : A monocarboxylic acid that is thyroacetic acid carrying four iodo substituents at positions 3, 3', 5 and 5'.		2.44202-halophenol;
aromatic ether;
iodophenol;
monocarboxylic acid		apoptosis inducer;
human metabolite;
thyroid hormone
fluorodeoxyglucose f18
Fluorodeoxyglucose F18: The compound is given by intravenous injection to do POSITRON-EMISSION TOMOGRAPHY for the assessment of cerebral and myocardial glucose metabolism in various physiological or pathological states including stroke and myocardial ischemia. It is also employed for the detection of malignant tumors including those of the brain, liver, and thyroid gland. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1162)		2.41102-deoxy-2-((18)F)fluoro-D-glucose;
2-deoxy-2-fluoro-aldehydo-D-glucose
3,5-dimethyl-3'-isopropyl-l-thyronine
3,5-dimethyl-3'-isopropyl-L-thyronine: RN given refers to (L)-isomer		2.4120
caprylates
Caprylates: Derivatives of caprylic acid. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain a carboxy terminated eight carbon aliphatic structure.. octanoate : A straight-chain saturated fatty acid anion that is the conjugate base of octanoic acid (caprylic acid); believed to block adipogenesis.		2.2510fatty acid anion 8:0;
straight-chain saturated fatty acid anion		human metabolite;
Saccharomyces cerevisiae metabolite
3,5-diiodothyronine
3,5-diiodothyronine: RN given refers to parent cpd without isomeric designation; structure		4.1320organonitrogen compound;
organooxygen compound
proline
Proline: A non-essential amino acid that is synthesized from GLUTAMIC ACID. It is an essential component of COLLAGEN and is important for proper functioning of joints and tendons.. proline : An alpha-amino acid that is pyrrolidine bearing a carboxy substituent at position 2.		2.4110amino acid zwitterion;
glutamine family amino acid;
L-alpha-amino acid;
proline;
proteinogenic amino acid		algal metabolite;
compatible osmolytes;
Escherichia coli metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
3,5-diiodothyropropionic acid
3,5-diiodothyropropionic acid: a cardiotonic thyroid hormone analog. 3,5-diiodothyropropionic acid : A monocarboxylic acid that is (4-hydroxy-3,5-diiodophenyl)propanoic acid in which the phenolic hydroxy group has been replaced by a 4-hydroxyphenyl group. An ionotropic analogue of L-thyroxine.		3.6120aromatic ether;
monocarboxylic acid;
organoiodine compound;
phenols
campesterol
campesterol: RN refers to (3beta,24R)-isomer; structure		2.1103beta-hydroxy-Delta(5)-steroid;
3beta-sterol;
C28-steroid;
phytosterols		mouse metabolite
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		3.6120divalent inorganic anion;
phosphite ion
monoiodotyrosine
Monoiodotyrosine: A product from the iodination of tyrosine. In the biosynthesis of thyroid hormones (THYROXINE and TRIIODOTHYRONINE), tyrosine is first iodized to monoiodotyrosine.. iodotyrosine : A tyrosine derivative which has at least one iodo-substituent on the benzyl moiety.. monoiodotyrosine : An iodotyrosine carrying a single iodo substituent.. 3-iodo-L-tyrosine : The monoiodotyrosine that is L-tyrosine carrying an iodo-substituent at position C-3 of the benzyl group.		3.1810amino acid zwitterion;
L-tyrosine derivative;
monoiodotyrosine;
non-proteinogenic L-alpha-amino acid		EC 1.14.16.2 (tyrosine 3-monooxygenase) inhibitor;
human metabolite;
mouse metabolite
sodium perchlorate
sodium perchlorate : An inorganic sodium salt comprising equal numbers of sodium and perchlorate ions.		2.1110inorganic sodium salt
methimazole
Methimazole: A thioureylene antithyroid agent that inhibits the formation of thyroid hormones by interfering with the incorporation of iodine into tyrosyl residues of thyroglobulin. This is done by interfering with the oxidation of iodide ion and iodotyrosyl groups through inhibition of the peroxidase enzyme.. methimazole : A member of the class of imidazoles that it imidazole-2-thione in which a methyl group replaces the hydrogen which is attached to a nitrogen.		2.11101,3-dihydroimidazole-2-thionesantithyroid drug
sirolimus
Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.		2.2110antibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol		antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
cysteine
Cysteine: A thiol-containing non-essential amino acid that is oxidized to form CYSTINE.. L-cysteinium : The L-enantiomer of cysteinium.. cysteine : A sulfur-containing amino acid that is propanoic acid with an amino group at position 2 and a sulfanyl group at position 3.		2.0210cysteiniumfundamental metabolite
thyronines
Thyronines: A group of metabolites derived from THYROXINE and TRIIODOTHYRONINE via the peripheral enzymatic removal of iodines from the thyroxine nucleus. Thyronine is the thyroxine nucleus devoid of its four iodine atoms.. thyronine : A tyrosine derivative where the phenolic hydrogen of tyrosine is substituted by 4-hydroxyphenyl.		3.3510thyronine
kb 141
KB 141: an anticholesteremic agent; structure in first source		6.7890
cgs 23425
CGS 23425: structure given in first source		2.4520
3-iodothyronamine
3-iodothyronamine: a thyroid hormone derivative that may be involved in a fast response signaling pathway; structure in first source		3.3510aromatic ether
kb 2115
3-((3,5-dibromo-4-(4-hydroxy-3-(1-methylethyl)phenoxy)phenyl)amino)-3-oxopropanoic acid: a thyroid hormone receptor agonist with anticholesteremic activity		6.28110
phytosterols
Phytosterols: A class of organic compounds known as sterols or STEROIDS derived from plants.. phytosterols : Sterols similar to cholesterol which occur in plants and vary only in carbon side chains and/or presence or absence of a double bond.		2.110
mgl-3196
resmetirom: a thyroid hormone receptor-beta agonist		3.9730
triiodothyronine, reverse
Triiodothyronine, Reverse: A metabolite of THYROXINE, formed by the peripheral enzymatic monodeiodination of T4 at the 5 position of the inner ring of the iodothyronine nucleus.. 3,3',5'-triiodo-L-thyronine zwitterion : Zwitterionic form of 3,3',5'-triiodo-L-thyronine.		3.18103,3',5'-triiodothyronine;
amino acid zwitterion
ConditionIndicatedRelationship StrengthStudiesTrials
Glial Cell Tumors
[description not available]		01.9510
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		01.9510
Neuroblastoma
A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)		01.9510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		04.85110
Elevated Cholesterol
[description not available]		02.7130
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		02.7130
Dyslipidemia
[description not available]		05.7480
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		05.7480
Addison Disease and Cerebral Sclerosis
[description not available]		03.0640
Adrenoleukodystrophy
An X-linked recessive disorder characterized by the accumulation of saturated very long chain fatty acids in the LYSOSOMES of ADRENAL CORTEX and the white matter of CENTRAL NERVOUS SYSTEM. This disease occurs almost exclusively in the males. Clinical features include the childhood onset of ATAXIA; NEUROBEHAVIORAL MANIFESTATIONS; HYPERPIGMENTATION; ADRENAL INSUFFICIENCY; SEIZURES; MUSCLE SPASTICITY; and DEMENTIA. The slowly progressive adult form is called adrenomyeloneuropathy. The defective gene ABCD1 is located at Xq28, and encodes the adrenoleukodystrophy protein (ATP-BINDING CASSETTE TRANSPORTERS).		15.6580
Colorectal Cancer
[description not available]		02.4110
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		02.4110
Delayed Effects, Prenatal Exposure
[description not available]		02.610
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		02.4920
Autism Spectrum Disorder
Wide continuum of associated cognitive and neurobehavioral disorders, including, but not limited to, three core-defining features: impairments in socialization, impairments in verbal and nonverbal communication, and restricted and repetitive patterns of behaviors. (from DSM-V)		02.610
Deficiency, Mental
[description not available]		02.610
Intellectual Disability
Subnormal intellectual functioning which originates during the developmental period. This has multiple potential etiologies, including genetic defects and perinatal insults. Intelligence quotient (IQ) scores are commonly used to determine whether an individual has an intellectual disability. IQ scores between 70 and 79 are in the borderline range. Scores below 67 are in the disabled range. (from Joynt, Clinical Neurology, 1992, Ch55, p28)		02.610
Injury, Ischemia-Reperfusion
[description not available]		02.610
Spermatic Cord Torsion
The twisting of the SPERMATIC CORD due to an anatomical abnormality that left the TESTIS mobile and dangling in the SCROTUM. The initial effect of testicular torsion is obstruction of venous return. Depending on the duration and degree of cord rotation, testicular symptoms range from EDEMA to interrupted arterial flow and testicular pain. If blood flow to testis is absent for 4 to 6 h, SPERMATOGENESIS may be permanently lost.		02.610
Reperfusion Injury
Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.		02.610
Thyroid Cancer, Anaplastic
[description not available]		02.610
Cancer of the Thyroid
[description not available]		02.610
Aggression
Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism.		02.610
Thyroid Neoplasms
Tumors or cancer of the THYROID GLAND.		02.610
Thyroid Carcinoma, Anaplastic
An aggressive THYROID GLAND malignancy which generally occurs in IODINE-deficient areas in people with previous thyroid pathology such as GOITER. It is associated with CELL DEDIFFERENTIATION of THYROID CARCINOMA (e.g., FOLLICULAR THYROID CARCINOMA; PAPILLARY THYROID CANCER). Typical initial presentation is a rapidly growing neck mass which upon metastasis is associated with DYSPHAGIA; NECK PAIN; bone pain; DYSPNEA; and NEUROLOGIC DEFICITS.		02.610
Fatty Liver, Nonalcoholic
[description not available]		04.6350
Central Nervous System Disease
[description not available]		03.1710
Liver Dysfunction
[description not available]		03.9820
Central Nervous System Diseases
Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.		03.1710
Liver Diseases
Pathological processes of the LIVER.		03.9820
Non-alcoholic Fatty Liver Disease
Fatty liver finding without excessive ALCOHOL CONSUMPTION.		04.6350
Lipid Metabolism, Inborn Error
[description not available]		02.2510
Bile Duct Obstruction, Intrahepatic
[description not available]		02.2510
Cholestasis, Intrahepatic
Impairment of bile flow due to injury to the HEPATOCYTES; BILE CANALICULI; or the intrahepatic bile ducts (BILE DUCTS, INTRAHEPATIC).		02.2510
Clinically Isolated CNS Demyelinating Syndrome
[description not available]		02.3110
Allergic Encephalomyelitis
[description not available]		02.7620
Nerve Degeneration
Loss of functional activity and trophic degeneration of nerve axons and their terminal arborizations following the destruction of their cells of origin or interruption of their continuity with these cells. The pathology is characteristic of neurodegenerative diseases. Often the process of nerve degeneration is studied in research on neuroanatomical localization and correlation of the neurophysiology of neural pathways.		02.3110
Demyelinating Diseases
Diseases characterized by loss or dysfunction of myelin in the central or peripheral nervous system.		02.3110
Amyloid Neuropathy Type 1
[description not available]		02.3110
Amyloid Neuropathies, Familial
Inherited disorders of the peripheral nervous system associated with the deposition of AMYLOID in nerve tissue. The different clinical types based on symptoms correspond to the presence of a variety of mutations in several different proteins including transthyretin (PREALBUMIN); APOLIPOPROTEIN A-I; and GELSOLIN.		02.3110
Hepatocellular Carcinoma
[description not available]		03.7730
Cancer of Liver
[description not available]		03.7730
Carcinoma, Hepatocellular
A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.		03.7730
Liver Neoplasms
Tumors or cancer of the LIVER.		03.7730
Hepatic Insufficiency
Conditions in which the LIVER functions fall below the normal ranges. Severe hepatic insufficiency may cause LIVER FAILURE or DEATH. Treatment may include LIVER TRANSPLANTATION.		02.1510
Central Hypothyroidism
[description not available]		04.2160
Hypothyroidism
A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.		04.2160
Obesity
A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).		03.9140
Atherogenesis
[description not available]		04.3940
Apolipoprotein B-100, Familial Defective
[description not available]		02.2110
Hyperlipoproteinemia Type II
A group of familial disorders characterized by elevated circulating cholesterol contained in either LOW-DENSITY LIPOPROTEINS alone or also in VERY-LOW-DENSITY LIPOPROTEINS (pre-beta lipoproteins).		02.2110
Atherosclerosis
A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.		04.3940
MS (Multiple Sclerosis)
[description not available]		02.2110
Multiple Sclerosis
An autoimmune disorder mainly affecting young adults and characterized by destruction of myelin in the central nervous system. Pathologic findings include multiple sharply demarcated areas of demyelination throughout the white matter of the central nervous system. Clinical manifestations include visual loss, extra-ocular movement disorders, paresthesias, loss of sensation, weakness, dysarthria, spasticity, ataxia, and bladder dysfunction. The usual pattern is one of recurrent attacks followed by partial recovery (see MULTIPLE SCLEROSIS, RELAPSING-REMITTING), but acute fulminating and chronic progressive forms (see MULTIPLE SCLEROSIS, CHRONIC PROGRESSIVE) also occur. (Adams et al., Principles of Neurology, 6th ed, p903)		02.2110
Liver Steatosis
[description not available]		05.2740
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		02.4920
Compensatory Hyperinsulinemia
A GLUCOSE-induced HYPERINSULINEMIA, a marker of insulin-resistant state. It is a mechanism to compensate for reduced sensitivity to insulin.		02.0810
Insulin Sensitivity
[description not available]		02.520
Fatty Liver
Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.		05.2740
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		02.4920
Hyperinsulinism
A syndrome with excessively high INSULIN levels in the BLOOD. It may cause HYPOGLYCEMIA. Etiology of hyperinsulinism varies, including hypersecretion of a beta cell tumor (INSULINOMA); autoantibodies against insulin (INSULIN ANTIBODIES); defective insulin receptor (INSULIN RESISTANCE); or overuse of exogenous insulin or HYPOGLYCEMIC AGENTS.		02.0810
Insulin Resistance
Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.		02.520
Aura
[description not available]		02.110
Epilepsy
A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)		02.110
Hypertriglyceridemia
A condition of elevated levels of TRIGLYCERIDES in the blood.		02.110
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		03.6730
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		02.1310
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		02.1310
Body Weight
The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.		02.7330
Arteriosclerosis
Thickening and loss of elasticity of the walls of ARTERIES of all sizes. There are many forms classified by the types of lesions and arteries involved, such as ATHEROSCLEROSIS with fatty lesions in the ARTERIAL INTIMA of medium and large muscular arteries.		02.9610
Alloxan Diabetes
[description not available]		02.0810