Compounds > 2164u90
Page last updated: 2024-12-11

2164u90

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

Description

2164U90: a potent inhibitor of the ileal bile acid active transport system; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9841699
CHEMBL ID2074988
SCHEMBL ID9961463
MeSH IDM0251260

Synonyms (8)

Synonym
bdbm50390996
CHEMBL2074988 ,
SCHEMBL9961463
(3r,5r)-3-butyl-3-ethyl-5-phenyl-4,5-dihydro-2h-1lambda6,4-benzothiazepine 1,1-dioxide
2164u90
(3r,5r)-3-butyl-3-ethyl-5-phenyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine 1,1-dioxide
152802-07-8
PD128842

Research Excerpts

Overview

2164U90 is a benzothiazepine-based competitive inhibitor of bile acid transport. K(i) values of approximately 10 and 0.068 microM for the homologous human and mouse apical transporters, respectively.

ExcerptReferenceRelevance
"2164U90 is a benzothiazepine-based competitive inhibitor of bile acid transport with K(i) values of approximately 10 and 0.068 microM for the homologous human and mouse apical transporters, respectively."( Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor.
Björquist, A; Hallén, S; Ostlund-Lindqvist, AM; Sachs, G, 2002)		1.04

Actions

ExcerptReferenceRelevance
"2164U90 did not inhibit sodium-dependent glucose transport by monkey jejunal brush border membrane vesicles, indicating that 2164U90 may be specific for the bile acid transporter."( Inhibition of ileal sodium-dependent bile acid transport by 2164U90.
Brieaddy, LE; Lewis, MC; Root, C; Smith, CD; Winegar, DA, 1995)		1.25

Dosage Studied

ExcerptRelevanceReference
" IBAT inhibitors, a new class of hypocholesterolemic drugs may be used alone or in combination with HMG-CoA reductase inhibitors in the treatment of hypercholesterolemia with low dosage and high compliance."( [Hypolipidemic drugs--ileal Na+/bile acid cotransporter inhibitors (S-8921 etc)].
Ichihashi, T, 2002)		0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Ileal sodium/bile acid cotransporterMus musculus (house mouse)Ki0.06800.06800.06800.0680AID679714
Ileal sodium/bile acid cotransporterHomo sapiens (human)Ki10.00003.30006.400010.0000AID679690
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (4)

Processvia Protein(s)Taxonomy
sodium ion transportIleal sodium/bile acid cotransporterHomo sapiens (human)
response to bacteriumIleal sodium/bile acid cotransporterHomo sapiens (human)
bile acid and bile salt transportIleal sodium/bile acid cotransporterHomo sapiens (human)
transmembrane transportIleal sodium/bile acid cotransporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
protein bindingIleal sodium/bile acid cotransporterHomo sapiens (human)
bile acid:sodium symporter activityIleal sodium/bile acid cotransporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
plasma membraneIleal sodium/bile acid cotransporterHomo sapiens (human)
microvillusIleal sodium/bile acid cotransporterHomo sapiens (human)
apical plasma membraneIleal sodium/bile acid cotransporterHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID679690TP_TRANSPORTER: inhibition of Taurocholate accumulation in ASBT-expressing HEK293 cells2002Biochemistry, Dec-17, Volume: 41, Issue:50
Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor.
AID679714TP_TRANSPORTER: inhibition of Taurocholate accumulation in ASBT-expressing HEK293 cells2002Biochemistry, Dec-17, Volume: 41, Issue:50
Identification of a region of the ileal-type sodium/bile acid cotransporter interacting with a competitive bile acid transport inhibitor.
[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's2 (40.00)18.2507
2000's3 (60.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.50

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 Index12.50 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.29 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.50)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (20.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (80.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
serine
Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.		2.0110L-alpha-amino acid;
proteinogenic amino acid;
serine family amino acid;
serine zwitterion;
serine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
valine
Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.		2.0110L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
pyruvate family amino acid;
valine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
threonine
Threonine: An essential amino acid occurring naturally in the L-form, which is the active form. It is found in eggs, milk, gelatin, and other proteins.. threonine : An alpha-amino acid in which one of the hydrogens attached to the alpha-carbon of glycine is substituted by a 1-hydroxyethyl group.		2.0110amino acid zwitterion;
aspartate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
threonine		algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
taurocholic acid
Taurocholic Acid: The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.. taurocholate : An organosulfonate oxoanion that is the conjugate base of taurocholic acid.. taurocholic acid : A bile acid taurine conjugate of cholic acid that usually occurs as the sodium salt of bile in mammals.		2.9140amino sulfonic acid;
bile acid taurine conjugate		human metabolite
2-naphthol
2-naphthol: RN given refers to parent cpd. 2-naphthol : A naphthol carrying a hydroxy group at position 2.. naphthols : Any hydroxynaphthalene derivative that has a single hydroxy substituent.		3.1110naphtholantinematodal drug;
genotoxin;
human urinary metabolite;
human xenobiotic metabolite;
mouse metabolite;
radical scavenger
glycocholic acid
Glycocholic Acid: The glycine conjugate of CHOLIC ACID. It acts as a detergent to solubilize fats for absorption and is itself absorbed.. glycocholic acid : A bile acid glycine conjugate having cholic acid as the bile acid component.. glycocholate : A cholanic acid conjugate anion that is the conjugate base of glycocholic acid, obtained by deprotonation of the carboxy group; major species at pH 7.3.		210bile acid glycine conjugatehuman metabolite
(2-(trimethylammonium)ethyl)methanethiosulfonate
(2-(trimethylammonium)ethyl)methanethiosulfonate: RN given for bromide; used in dopamine analysis		2.0110
s 8921
S 8921: inhibits bile acid transport; structure given in first source		3.1110
ouabain
Ouabain: A cardioactive glycoside consisting of rhamnose and ouabagenin, obtained from the seeds of Strophanthus gratus and other plants of the Apocynaceae; used like DIGITALIS. It is commonly used in cell biological studies as an inhibitor of the NA(+)-K(+)-EXCHANGING ATPASE.. cardiac glycoside : Steroid lactones containing sugar residues that act on the contractile force of the cardiac muscles.. ouabain : A steroid hormone that is a multi-hydroxylated alpha-L-rhamnosyl cardenoloide. It binds to and inhibits the plasma membrane Na(+)/K(+)-ATPase (sodium pump). It has been isolated naturally from Strophanthus gratus.		21011alpha-hydroxy steroid;
14beta-hydroxy steroid;
5beta-hydroxy steroid;
alpha-L-rhamnoside;
cardenolide glycoside;
steroid hormone		anti-arrhythmia drug;
cardiotonic drug;
EC 2.3.3.1 [citrate (Si)-synthase] inhibitor;
EC 3.1.3.41 (4-nitrophenylphosphatase) inhibitor;
EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor;
EC 3.6.3.9 (Na(+)/K(+)-transporting ATPase) inhibitor;
ion transport inhibitor;
plant metabolite
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.		2.0110cysteiniumfundamental metabolite
cholestyramine resin
Cholestyramine Resin: A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.		1.9810
ConditionIndicatedRelationship StrengthStudiesTrials
Elevated Cholesterol
[description not available]		02.9210
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.		02.9210