Page last updated: 2024-12-10

susalimod

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

Description

susalimod: analogue of sulphasalazine, was designed for use in the treatment of rheumatoid arthritis [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3086668
CHEMBL ID1614646
SCHEMBL ID1229340
MeSH IDM0306740

Synonyms (21)

Synonym
susalimod
2-hydroxy-5-[2-[4-[(3-methylpyridin-2-yl)sulfamoyl]phenyl]ethynyl]benzoic acid
CHEMBL1614646 ,
i5mpg6f043 ,
unii-i5mpg6f043
149556-49-0
5-((p-((3-methyl-2-pyridyl)sulfamoyl)phenyl)ethynyl)salicylic acid
susalimod [inn]
bdbm50355009
2-hydroxy-5-[[4-[(3-methyl-2-pyridinylamino)sulfonyl]phenyl]ethynyl]benzoic acid
2-hydroxy -5-[[4-[(3-methyl-2-pyridinylamino)sulfonyl]phenyl]ethynyl]benzoic acid
WJLQPSZXCOYTHS-UHFFFAOYSA-N
2-hydroxy-5-[[4-[(3-methyl-2-pyridinylamino)sulfonyl]phenyl]ethynyl]-benzoic acid
2-hydroxy -5-[[4-[(3-methyl-2-pyridinylamino)sulfonyl]phenyl]ethynyl]-benzoic acid
SCHEMBL1229340
DTXSID80164336
Q27280478
D93397
2-hydroxy-5-((4-(n-(3-methylpyridin-2-yl)sulfamoyl)phenyl)ethynyl)benzoicacid
2-hydroxy-5-((4-(n-(3-methylpyridin-2-yl)sulfamoyl)phenyl)ethynyl)benzoic acid
AS-78435

Research Excerpts

Overview

Susalimod is a structural analogue of sulphasalazine, known to be extensively excreted in the bile in various animal species. It is used for inducing bile duct hyperplasia after long-term treatment of the dog.

ExcerptReferenceRelevance
"Susalimod is a structural analogue of sulphasalazine, known to be extensively excreted in the bile in various animal species and for inducing bile duct hyperplasia after long-term treatment of the dog with doses exceeding 25 mg kg(-1). "( Efficient biliary excretion of susalimod, probably via the bromosulphthalein carrier, studied in a chronic bile fistula model in dogs.
Bowald, S; Påhlman, I; Wilén, M, 1999
)
2.03

Pharmacokinetics

ExcerptReferenceRelevance
", a three-compartment pharmacokinetic model, including biliary excretion, and an indirect mechanistically based pharmacodynamic model."( Pharmacokinetic-pharmacodynamic modeling of the immunomodulating agent susalimod and experimentally induced tumor necrosis factor-alpha levels in the mouse.
Gozzi, P; Grönberg, A; Påhlman, I; Palmér, L; Persson, S, 1999
)
0.54
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cystine/glutamate transporterHomo sapiens (human)IC50 (µMol)70.00000.14001.14005.0000AID622159
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (34)

Processvia Protein(s)Taxonomy
glutathione metabolic processCystine/glutamate transporterHomo sapiens (human)
visual learningCystine/glutamate transporterHomo sapiens (human)
response to toxic substanceCystine/glutamate transporterHomo sapiens (human)
response to organic cyclic compoundCystine/glutamate transporterHomo sapiens (human)
L-cystine transportCystine/glutamate transporterHomo sapiens (human)
L-glutamate transmembrane transportCystine/glutamate transporterHomo sapiens (human)
ventricular system developmentCystine/glutamate transporterHomo sapiens (human)
striatum developmentCystine/glutamate transporterHomo sapiens (human)
adult behaviorCystine/glutamate transporterHomo sapiens (human)
regulation of neutrophil apoptotic processCystine/glutamate transporterHomo sapiens (human)
cellular response to oxidative stressCystine/glutamate transporterHomo sapiens (human)
glutathione transmembrane transportCystine/glutamate transporterHomo sapiens (human)
response to nicotineCystine/glutamate transporterHomo sapiens (human)
regulation of cell population proliferationCystine/glutamate transporterHomo sapiens (human)
regulation of melanin biosynthetic processCystine/glutamate transporterHomo sapiens (human)
lung alveolus developmentCystine/glutamate transporterHomo sapiens (human)
modulation of chemical synaptic transmissionCystine/glutamate transporterHomo sapiens (human)
regulation of synapse organizationCystine/glutamate transporterHomo sapiens (human)
regulation of protein transportCystine/glutamate transporterHomo sapiens (human)
response to redox stateCystine/glutamate transporterHomo sapiens (human)
limb developmentCystine/glutamate transporterHomo sapiens (human)
lens fiber cell differentiationCystine/glutamate transporterHomo sapiens (human)
platelet aggregationCystine/glutamate transporterHomo sapiens (human)
intracellular glutamate homeostasisCystine/glutamate transporterHomo sapiens (human)
L-glutamate import across plasma membraneCystine/glutamate transporterHomo sapiens (human)
negative regulation of ferroptosisCystine/glutamate transporterHomo sapiens (human)
dipeptide import across plasma membraneCystine/glutamate transporterHomo sapiens (human)
L-kynurenine transmembrane transportCystine/glutamate transporterHomo sapiens (human)
regulation of cellular response to oxidative stressCystine/glutamate transporterHomo sapiens (human)
regulation of cysteine metabolic processCystine/glutamate transporterHomo sapiens (human)
regulation of glutathione biosynthetic processCystine/glutamate transporterHomo sapiens (human)
regulation of AMPA glutamate receptor clusteringCystine/glutamate transporterHomo sapiens (human)
regulation of glutamate metabolic processCystine/glutamate transporterHomo sapiens (human)
amino acid transmembrane transportCystine/glutamate transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
protein bindingCystine/glutamate transporterHomo sapiens (human)
cystine:glutamate antiporter activityCystine/glutamate transporterHomo sapiens (human)
L-kynurenine transmembrane transporter activityCystine/glutamate transporterHomo sapiens (human)
L-amino acid transmembrane transporter activityCystine/glutamate transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
plasma membraneCystine/glutamate transporterHomo sapiens (human)
cell surfaceCystine/glutamate transporterHomo sapiens (human)
membraneCystine/glutamate transporterHomo sapiens (human)
brush border membraneCystine/glutamate transporterHomo sapiens (human)
microvillus membraneCystine/glutamate transporterHomo sapiens (human)
apical part of cellCystine/glutamate transporterHomo sapiens (human)
astrocyte projectionCystine/glutamate transporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (9)

Assay IDTitleYearJournalArticle
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID622159Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Inhibition of xc⁻ transporter-mediated cystine uptake by sulfasalazine analogs.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (60.00)18.2507
2000's1 (20.00)29.6817
2010's1 (20.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]