Compounds > milfasartan
Page last updated: 2024-11-10

milfasartan

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

Description

milfasartan: angiotensin I receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3047757
CHEMBL ID429847
SCHEMBL ID489256
MeSH IDM0519312

Synonyms (19)

Synonym
milfasartan
bdbm50241491
2-{4-butyl-2-methyl-6-oxo-5-[2''-(1h-tetrazol-5-yl)-biphenyl-4-ylmethyl]-6h-pyrimidin-1-ylmethyl}-thiophene-3-carboxylic acid methyl ester
CHEMBL429847 ,
L001493
methyl 2-[[4-butyl-2-methyl-6-oxo-5-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-1-yl]methyl]thiophene-3-carboxylate
148564-47-0
8ual5421cl ,
milfasartan [inn]
unii-8ual5421cl
methyl 2-((4-butyl-2-methyl-6-oxo-5-(p-(o-1h-tetrazol-5-ylphenyl)benzyl)-1(6h)-pyrimidinyl)methyl)-3-thiophenecarboxylate
SCHEMBL489256
2,3,3a,4,7,7a-hexahydro-1h-indene-2-carboxylicacid
DTXSID70164007
3-thiophenecarboxylic acid, 2-[[4-butyl-2-methyl-6-oxo-5-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1(6h)-pyrimidinyl]methyl]-, methyl ester
6-butyl-2-methyl-3-[[3-(methoxycarbonyl)thien-2-yl]methyl]- -5-[[2'-(1h-tetrazol-5-yl)]][1,1'-biphenyl)-4-yl]methyl]pyrimidin-4(3h)-one
Q27271019
SB60394
AKOS040748918
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1A angiotensin II receptor Rattus norvegicus (Norway rat)Ki0.00140.00020.10251.7000AID37973
Type-1B angiotensin II receptorRattus norvegicus (Norway rat)Ki0.00140.00020.05211.1000AID37973
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (3)

Processvia Protein(s)Taxonomy
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorBos taurus (cattle)
regulation of vasoconstrictionType-1 angiotensin II receptorBos taurus (cattle)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
angiotensin type I receptor activityType-1 angiotensin II receptorBos taurus (cattle)
angiotensin type II receptor activityType-1 angiotensin II receptorBos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (10)

Assay IDTitleYearJournalArticle
AID174940Time duration was determined from onset of the action till no response after (i.v.) administration of 1 mg/kg in anesthetized, ganglion blocked, A II- infused rat1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID177661Effect on pressure response to angiotensin II receptor (AII) after (i.v.) administration of 1 mg/kg in anesthetized, ganglion blocked, AII-infused rat in vivo1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID167541Compound was tested for its antagonistic activity against angiotensin II-induced contractions in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID177662Effect on pressure response to angiotensin II receptor (AII) after intradermally administration of 1 mg/kg in anesthetized, ganglion blocked, A II- infused rat was determined in vivo1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID320852Antagonist activity at rat AT1 receptor expressed in CHO cells assessed as angiotensin 2-evoked increase in intracellular calcium level2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Selenosartans: novel selenophene analogues of milfasartan and eprosartan.
AID37527Binding affinity was evaluated towards Angiotensin II receptor, type 1 in rabbit aorta1996Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
AID37973Displacement of [3H]angiotensin II from Angiotensin II type 1 receptor in rat adrenal cortical membrane1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID38142Binding affinity towards Angiotensin II type 2 receptor in bovine cerebellar cortical membranes; Inactive1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
AID568917Binding affinity to angiotensin AT1 receptor in rat adrenal cortical membranes2010Bioorganic & medicinal chemistry, Dec-15, Volume: 18, Issue:24
Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
AID174941Time duration was determined from onset of the action till no response after intradermal administration of 1 mg/kg in anesthetized, ganglion blocked, A II- infused rat1995Journal of medicinal chemistry, Nov-24, Volume: 38, Issue:24
N-3-substituted pyrimidinones as potent, orally active, AT1 selective angiotensin II receptor antagonists.
[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's1 (20.00)29.6817
2010's2 (40.00)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: 12.58

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 Index12.58 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (40.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (60.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
candesartan cilexetil
candesartan cilexetil: a prodrug which is metabolized to an active form candesartan to exert its biological effects		4.0320biphenyls
candesartan
candesartan: a nonpeptide angiotensin II receptor antagonist. candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension.		4.0320benzimidazolecarboxylic acid;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
avapro
Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.		4.0320azaspiro compound;
biphenylyltetrazole		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
losartan
Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position		4.330biphenylyltetrazole;
imidazoles		angiotensin receptor antagonist;
anti-arrhythmia drug;
antihypertensive agent;
endothelin receptor antagonist
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		2.4620mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
dup 532
DuP 532: angiotensin I receptor antagonist		4.0320
valsartan
Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.		4.0320biphenylyltetrazole;
monocarboxylic acid amide;
monocarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
tasosartan
tasosartan: angiotensin II antagonist; structure given in first source		4.0320biphenyls
telmisartan
Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION.. telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension.		3.1510benzimidazoles;
biphenyls;
carboxybiphenyl		angiotensin receptor antagonist;
antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
environmental contaminant;
xenobiotic
gr 117289
GR 117289: angiotensin AT1 receptor antagonist; structure given in first source. zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued).		4.03201-benzofurans;
biaryl;
imidazolyl carboxylic acid;
monocarboxylic acid;
organobromine compound;
organochlorine compound;
tetrazoles		angiotensin receptor antagonist;
antihypertensive agent
exp3174
losartan carboxylic acid: structure given in first source. losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid.		4.330biphenylyltetrazole;
imidazoles;
organochlorine compound		metabolite
exp7711
EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source		3.4920
bibs 39
BIBS 39: structure given in first source; angiotensin II receptor antagonist		3.0910
sc 51316
SC 51316: structure given in first source; an angiotensin II receptor antagonist		3.1510
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3h-imidazo(4,5-b)pyridine
3-((2'-carboxybiphenyl-4-yl)methyl)-2-cyclopropyl-7-methyl-3H-imidazo(4,5-b)pyridine: a non-peptide angiotensin II-receptor antagonist; structure given in first source		4.0320
a 81988
A 81988: angiotensin II antagonist selective for type 1 receptors		4.0320
bibs 222
BIBS 222: structure given in first source; angiotensin II receptor antagonist		3.0910
ici d8731
ICI D8731: structure given in first source; an angiotensin II receptor antagonist		4.0320
forasartan
forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure. forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension.		4.0320benzenes;
pyridines;
tetrazoles;
triazoles		angiotensin receptor antagonist;
antihypertensive agent
up 269-6
UP 269-6: structure given in first source; angiotensin receptor antagonist		4.0320
mk 996
MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source		4.0320
olmesartan
olmesartan: an active metabolite of CS 866		3.1510biphenylyltetrazoleangiotensin receptor antagonist;
antihypertensive agent
me 3221
ME 3221: an angiotensin II receptor antagonist; structure given in first source		4.0320
l 158809
L 158809: RN & structure given in first source; angiotensin receptor antagonist		4.0320
cv 11194
CV 11194: structure given in first source; an angiotensin II receptor antagonist		3.1510
dmp 811
DMP 811: angiotensin II receptor antagonist; structure given in first source		4.0320
eprosartan
eprosartan: angiotensin II receptor antagonist. eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure.		9.3230dicarboxylic acid;
imidazoles;
thiophenes		angiotensin receptor antagonist;
antihypertensive agent;
environmental contaminant;
xenobiotic
exp 655
[no description available]		3.0910
sulfur
Sulfur: An element that is a member of the chalcogen family. It has an atomic symbol S, atomic number 16, and atomic weight [32.059; 32.076]. It is found in the amino acids cysteine and methionine.		2.0410chalcogen;
nonmetal atom		macronutrient
l 162313
L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95		3.0910
pratosartan
pratosartan: angiotensin II type 1 receptor blocker		4.0320biphenylyltetrazoleantihypertensive agent
l 163491
L 163491: structure given in first source		3.0910
ema401
[no description available]		3.0910
azilsartan
azilsartan: an angiotensin type 1 receptor blocker; receptor blocker. azilsartan : A benzimidazolecarboxylic acid that is benzimidazole-7-carboxylic acid substituted at position 2 by a methoxy group and at position 1 by a 2'-[(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl group. Used (as the prodrug, azilsartan medoxomil) for treatment of hypertension.		3.15101,2,4-oxadiazole;
aromatic ether;
benzimidazolecarboxylic acid		angiotensin receptor antagonist;
antihypertensive agent
ConditionIndicatedRelationship StrengthStudiesTrials
Blood Pressure, High
[description not available]		01.9810
Hypertension
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.		01.9810
Extravascular Hemolysis
[description not available]		02.0710
Hemolysis
The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.		02.0710