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ro 48-5033

Description

Ro 48-5033: structure in first source [MeSH]

Cross-References

ID SourceID
PubMed CID6426755
CHEMBL ID3901721
SCHEMBL ID7205072
MeSH IDM0332079

Synonyms (27)

Synonym
n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]-4-(1-hydroxy-2-methylpropan-2-yl)benzenesulfonamide
4-(2-hydroxy-1,1-dimethylethyl)-n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2'-bipyrimidin]-4-yl]-benzenesulfonamide
FT-0669430
unii-vz7ynj87xh
ro 48-5033
hydroxybosentan
ro 48-8634
benzenesulfonamide, 4-(2-hydroxy-1,1-dimethylethyl)-n-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)(2,2'-bipyrimidin)-4-yl)-
vz7ynj87xh ,
253688-60-7
hydroxy bosentan
bosentan metabolite ro 48-5033
SCHEMBL7205072
FAJQMBCLPZWTQJ-UHFFFAOYSA-N
n-[4-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)pyrimidin-6-yl]4-(2-hydroxy-1,1-dimethylethyl)benzenesulphonamide
n-[4-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)pyrimidin-6-yl]-4-(2-hydroxy-1,1-dimethylethyl)benzenesulphonamide
AKOS030239680
J-015960
CHEMBL3901721
FT-0669431
FT-0669432
CS-0081840
HY-121385
BCP15832
hydroxybosentan pound>>ro 48-5033 pound>>ro 48-8634 pound>>bosentan metabolite ro 48-5033
4-(2-hydroxy-1,1-dimethylethyl)-n-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)(2,2'-bipyrimidin)-4-yl)benzenesulfonamide
4-(2-hydroxy-1,1-dimethylethyl)-n-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2?-bipyrimidin]-4-yl]-benzenesulfonamide

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1323162Drug level in human liver microsomes treated with bosentan at 5 uM in presence of NADPH after 30 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254Metabolism study and biological evaluation of bosentan derivatives.
AID1323173Retention time of the compound2016European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254Metabolism study and biological evaluation of bosentan derivatives.
AID1323149Drug level assessed as human recombinant CYP3A4-mediated compound formation treated with bosentan at 5 uM in presence of NADPH after 30 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254Metabolism study and biological evaluation of bosentan derivatives.
AID1323171Drug level assessed as human recombinant CYP2C9-mediated compound formation treated with bosentan at 5 uM in presence of NADPH after 30 mins by LC-MS/MS analysis2016European journal of medicinal chemistry, Oct-04, Volume: 121ISSN: 1768-3254Metabolism study and biological evaluation of bosentan derivatives.

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (16.67)18.2507
2000's2 (33.33)29.6817
2010's3 (50.00)24.3611
2020's0 (0.00)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (33.33%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other4 (66.67%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
bosentan anhydrousprimary alcohol;
pyrimidines;
sulfonamide
antihypertensive agent;
endothelin receptor antagonist
201620168.0low000010
bq 123cyclic peptide201620168.0low000010
ro 47-8634201620168.0high000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
estrone17-oxo steroid;
3-hydroxy steroid;
phenolic steroid;
phenols
antineoplastic agent;
bone density conservation agent;
estrogen;
human metabolite;
mouse metabolite
2007200717.0low000100
dehydroepiandrosterone sulfate17-oxo steroid;
steroid sulfate
EC 2.7.1.33 (pantothenate kinase) inhibitor;
human metabolite;
mouse metabolite
2007200717.0low000100
bosentan anhydrousprimary alcohol;
pyrimidines;
sulfonamide
antihypertensive agent;
endothelin receptor antagonist
1999201616.0high201220
estrone sulfate17-oxo steroid;
steroid sulfate
human metabolite;
mouse metabolite
2007200717.0low000100
ro 47-86341999201614.7high101020
warfarinbenzenes;
hydroxycoumarin;
methyl ketone
2007200717.0low000100
cyclosporine2007200717.0low000100
rifampincyclic ketal;
hydrazone;
N-iminopiperazine;
N-methylpiperazine;
rifamycins;
semisynthetic derivative;
zwitterion
angiogenesis inhibitor;
antiamoebic agent;
antineoplastic agent;
antitubercular agent;
DNA synthesis inhibitor;
EC 2.7.7.6 (RNA polymerase) inhibitor;
Escherichia coli metabolite;
geroprotector;
leprostatic drug;
neuroprotective agent;
pregnane X receptor agonist;
protein synthesis inhibitor
2007200717.0low000100
sildenafil citratecitrate saltEC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
2007200717.0low000100
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Liver Injury, Drug-Induced0201620168.0medium000010
Bilateral Headache01999199925.0medium101000
Chemical and Drug Induced Liver Injury0201620168.0medium000010
Cholera Infantum01999199925.0medium101000
Headache01999199925.0medium101000

Safety/Toxicity (2)

ArticleYear
Analysis of the Metabolic Pathway of Bosentan and of the Cytotoxicity of Bosentan Metabolites Based on a Quantitative Modeling of Metabolism and Transport in Sandwich-Cultured Human Hepatocytes.
Drug metabolism and disposition: the biological fate of chemicals, , Volume: 44, Issue:1
2016
Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers.
Journal of clinical pharmacology, , Volume: 39, Issue:7
1999

Pharmacokinetics (2)

ArticleYear
Comparative investigation of the pharmacokinetics of bosentan in Caucasian and Japanese healthy subjects.
Journal of clinical pharmacology, , Volume: 45, Issue:1
2005
Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers.
Journal of clinical pharmacology, , Volume: 39, Issue:7
1999

Bioavailability (1)

ArticleYear
Multiple-dose pharmacokinetics, safety, and tolerability of bosentan, an endothelin receptor antagonist, in healthy male volunteers.
Journal of clinical pharmacology, , Volume: 39, Issue:7
1999