Page last updated: 2024-11-06

lecimibide

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

Cross-References

ID SourceID
PubMed CID71355
CHEMBL ID274185
SCHEMBL ID49619
MeSH IDM0223505

Synonyms (31)

Synonym
lecimibide
3-(2,4-difluoro-phenyl)-1-[5-(4,5-diphenyl-1h-imidazol-2-ylsulfanyl)-pentyl]-1-heptyl-urea
bdbm50033969
D03735
lecimibide (usan)
130804-35-2
dup 128
CHEMBL274185 ,
dup-128
3-(2,4-difluorophenyl)-1-[5-[(4,5-diphenyl-1h-imidazol-2-yl)sulfanyl]pentyl]-1-heptylurea
unii-a7t248b302
3-(2,4-difluorophenyl)-1-(5-((4,5-diphenylimidazol-2-yl)thio)pentyl)-1-heptylurea
a7t248b302 ,
urea, n'-(2,4-difluorophenyl)-n-(5-((4,5-diphenyl-1h-imidazol-2-yl)thio)pentyl)-n-heptyl-
lecimibide [usan:inn]
3-(2,4-difluorophenyl)-1-[5-[(4,5-diphenylimidazol-2-yl)thio]pentyl]-1-heptylurea
lecimibide [inn]
lecimibide [usan]
lecimibide [who-dd]
SCHEMBL49619
n'-(2,4-difluorophenyl)-n-[5-(4,5 -diphenyl-1h-imidazol-2-ylthio)pentyl]-n-heptylurea
n'-(2,4-difluorophenyl)-n-[5-(4,5-diphenyl-1h-imidazol-2-ylthio)pentyl]-n-heptylurea
TVXOXGBTADZYCZ-UHFFFAOYSA-N
3-(2,4-difluorophenyl)-1-{5-[(4,5-diphenyl-1h-imidazol-2-yl)sulfanyl]pentyl}-1-heptylurea
3-(2,4-difluorophenyl)-1-[5-[[4,5-di(phenyl)-1h-imidazol-2-yl]sulfanyl]pentyl]-1-heptylurea
DTXSID80156751
dup128
Q1303494
3-(2,4-difluorophenyl)-1-(5-((4,5-diphenyl-1h-imidazol-2-yl)thio)pentyl)-1-heptylurea
GLXC-26601
AKOS040747027

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" We evaluated the effect of a potent, poorly absorbed ACAT inhibitor (DuP 128: N'-(2,4-difluorophenyl)-N-[5-(4,5-diphenyl-1H-imidazol-2-ylthio)pe ntyl]- N-heptylurea) on cholesterol absorption in a randomized trial."( Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans.
Connell, JM; Crouse, JR; Gillies, PJ; Hainer, JW; Hunt, TL; Jenkins, RM; Livak, KJ; Shand, DL; Terry, JG; Zyruk, H, 1994
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pathways (2)

PathwayProteinsCompounds
sterol:steryl ester interconversion (yeast)513
sterol:steryl ester interconversion513

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sterol O-acyltransferase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.28000.00580.66266.0000AID1396706; AID197093; AID31367
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.01000.00052.773925.1700AID197093
Sterol O-acyltransferase 1Mus musculus (house mouse)IC50 (µMol)0.91000.06000.59001.0000AID1396700; AID1396706
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1396706Inhibition of ACAT1 in mouse J774 cells assessed as reduction in esterified cholesterol accumulation after 18 hrs in presence of 25-hydroxycholesterol
AID168869Hypercholesterolemic activity in rats at a dose of 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.
AID31364Compound was evaluated for the Acyl coenzyme A:cholesterol acyltransferase inhibition using microsomes isolated from the livers of cholesterol fed rats.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.
AID181768Chronic 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.
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.
AID83670Evaluated for Syrian hamsters fed with 2.5% cholesterol-supplemented chow diet for 3 days1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
AID1396700Inhibition of ACAT1 in mouse J774 cells
AID31663Concentration required to inhibit 50% activity of Acyl coenzyme A:cholesterol acyltransferase 1 in vitro using rat liver microsome.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
AID83816Tested anti-hypercholesterolaemic value(AHV) is the ratio of observed reduction in serum cholesterol to difference between control and baseline levels x100 at 10 mg/kg/day dose1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
AID30893Acyl coenzyme A:cholesterol acyltransferase activity was determined in J774 macrophages by measuring the formation of labeled cholesteryl oleate (pmol/midmg) from [14C]oleoyl-CoA1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
AID1396703Inhibition of SOAT2 in New Zealand white rabbit intestinal microsomes assessed as reduction in cholesteryl oleate formation incubated for 5 mins in presence of [14C]-oleoyl-CoA and BSA complex by TLC method
AID31367In vitro inhibition of Acyl coenzyme A:cholesterol acyltransferase in rat hepatic microsomes1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
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.
AID181760Chronic 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.
AID83669Evaluated for Syrian hamsters fed with 0.8% cholesterol-supplemented chow diet for 7 days1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: synthesis and structure-activity relationship studies of a new series of trisubstituted imidazoles.
AID91773Concentration required to inhibit 50% activity of J774 macrophage cholesterol esterification1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
AID1396701Inhibition of ACAT2 in rat hepatic microsomes
AID181756Chronic 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.
AID1396702Inhibition of SOAT1 in arterial homogenates isolated from 1% cholesterol fed New Zealand white rabbit assessed as reduction in cholesteryl oleate formation incubated for 5 mins in presence of [14C]-oleoyl-CoA and BSA complex by TLC method
AID181748Chronic effect on preestablished dyslipidemia in rats for HDL-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.
AID168873Hypercholesterolemic activity in rats at a dose of 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.
AID181765Chronic 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.
AID181755Chronic effect on preestablished dyslipidemia in rats for nonHDL-C at 100 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.
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.
AID168871Hypercholesterolemic activity in rats at a dose of 100 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.
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.
AID181757Chronic 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.
AID181747Chronic effect on preestablished dyslipidemia in rats for HDL-C at 100 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.
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.
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.
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.
AID181764Chronic effect on preestablished dyslipidemia in rats for total cholesterol at 100 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.
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.
AID197093ACAT activity was determined in rat hepatic microsomes by measuring the formation of labeled cholesteryl oleate (pmol/midmg) from [14C]oleoyl-CoA1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
AID1396704Selectivity ratio of IC50 for inhibition of SOAT2 in New Zealand white rabbit intestinal microsomes to IC50 for inhibition of SOAT1 in arterial homogenates isolated from 1% cholesterol fed New Zealand white rabbit
AID30894Acyl coenzyme A:cholesterol acyltransferase inhibition in cell culture measured in murine IC-21 macrophages.1995Journal of medicinal chemistry, Mar-31, Volume: 38, Issue:7
Design, synthesis, and structure--activity relationship studies for a new imidazole series of J774 macrophage specific acyl-CoA:cholesterol acyltransferase (ACAT) inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's10 (71.43)18.2507
2000's3 (21.43)29.6817
2010's1 (7.14)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 (%)
Trials1 (7.14%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other12 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]