Compounds > pd 138142-15
Page last updated: 2024-11-12

pd 138142-15

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Cross-References

ID SourceID
PubMed CID10096821
CHEMBL ID25110
MeSH IDM0228545

Synonyms (7)

Synonym
carbamic acid, ((2,6-bis(1-methylethyl)phenoxy)sulfonyl)-, 2,6-bis(1-methylethyl)phenyl ester,monosodium salt
pd 138142-15
carbamic acid, (2,6-diisopropylphenoxysulfonyl)-, 2,6-diisopropylphenyl ester, sodium salt
cl-999
CHEMBL25110 ,
142878-84-0
sodium;[2,6-di(propan-2-yl)phenoxy]carbonyl-[2,6-di(propan-2-yl)phenoxy]sulfonylazanide
[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)
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC50 (µMol)4.00000.00600.98467.6000AID31218
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (44)

Assay IDTitleYearJournalArticle
AID21184Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 0 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID181754Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 10 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID168574Anti hypercholesterolemic activity in rats at a dose of 0.3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181759Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 30 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181749Chronic effect on preestablished dyslipidemia in rats for HDL-C at 1 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181745Chronic effect on preestablished dyslipidemia in rats for HDL-C at 0.3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID23496Partition coefficient was measured by the shake flask method at pH 7.4.1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID194914In vivo percent change in plasma cholesterol level was measured at a dose of 30 mg/Kg in rat and expressed as deltaTC; p < 0.011998Bioorganic & medicinal chemistry letters, Feb-03, Volume: 8, Issue:3
Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.
AID21178Solution Degradation Studies measured by compound unchanged at pH 0.4=50%1 M HCl/50% acetonitrile at 8 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID168872Hypercholesterolemic activity in rats at a dose of 3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID168868Hypercholesterolemic activity in rats at a dose of 1 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID45122Activity of compound in an intestine model using Caco-2 cells1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181762Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 1 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21187Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 4 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174746Acute in vivo activity measured by total plasma cholesterol concentration levels (TC) at 30 mg/kg dose1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID181761Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 0.3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181758Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21176Solution Degradation Studies measured by compound unchanged at pH 0.4=50%1 M HCl/50% acetonitrile at 24 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID181750Chronic effect on preestablished dyslipidemia in rats for HDL-C at 30 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID178588Effective dose to reduce plasma total cholesterol level by 50% of the control value in cholesterol fed rats1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.
AID31668In vitro inhibitory activity against acyl coenzyme A:cholesterol acyltransferase 1 in microsomes of rat liver1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID181752Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 0.3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181753Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 1 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21175Solution Degradation Studies measured by compound unchanged at pH 0.4=50%1 M HCl/50% acetonitrile at 2 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID31218In vitro inhibitory activity against Acyl coenzyme A:cholesterol acyltransferase (ACAT) in rabbit intestinal microsomes1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.
AID21177Solution Degradation Studies measured by compound unchanged at pH 0.4=50%1 M HCl/50% acetonitrile at 4 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID31057In vitro inhibition of ACAT by incubation with [1-14C]oleolyl-CoA and intestinal microsomes isolated from cholesterol-fed rabbits.1998Bioorganic & medicinal chemistry letters, Feb-03, Volume: 8, Issue:3
Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates.
AID168870Hypercholesterolemic activity in rats at a dose of 10 mg/kg was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21185Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 2 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174751Chronic in vivo activity was measured by the total cholesterol concentration levels in cholesterol fed rats1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID174734Chronic in vivo activity was measured by the concentration of high density lipoproteins (HDL) in cholesterol fed rats1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID176929Dose required to lower the plasma cholesterol by 50% in rats was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21186Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 24 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID181767Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 30 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181751Chronic effect on preestablished dyslipidemia in rats for HDL-C at 3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID31363Compound was evaluated for the Acyl coenzyme A:cholesterol acyltransferase inhibition using microsomes isolated from the livers of cholesterol fed rats1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181766Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 3 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID181746Chronic effect on preestablished dyslipidemia in rats for HDL-C at 10 kg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID21174Solution Degradation Studies measured by compound unchanged at pH 0.4=50%1 M HCl/50% acetonitrile at 0 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID174747Acute in vivo activity was measured by the total plasma cholesterol concentration levels(TC) at dose 3 mg/kg1996Journal of medicinal chemistry, Mar-15, Volume: 39, Issue:6
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
AID21188Solution Degradation Studies measured by compound unchanged at pH 6.4 = 50% water / 50% acetonitrile at 8 hours1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
AID181763Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 10 mg/kg of compound was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
AID132338Compound tested for inhibitory activity of foam cell formation in mouse peritoneal macrophages1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylureas.
AID168874Hypercholesterolemic activity in rats at a dose of 30 mg/kg was determined1994Journal of medicinal chemistry, Mar-04, Volume: 37, Issue:5
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
[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's5 (100.00)18.2507
2000's0 (0.00)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: 12.66

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 Index12.66 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.66)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
lecimibide
[no description available]		1.9810
cl 277082
CL 277082: structure given in first source		1.9910
avasimibe
[no description available]		2.420monoterpenoid
((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester
((2,6-bis(1-methylethyl)phenoxy)sulfonyl)carbamic acid 2,6-bis(1-methylethyl)phenyl ester: a water soluble inhibitor of ACAT; structure in first source		2.3920
ConditionIndicatedRelationship StrengthStudiesTrials
Elevated Cholesterol
[description not available]		01.9810
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.		01.9810
Necrosis
The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.		01.9910