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Details

Stereochemistry ACHIRAL
Molecular Formula C25H24FN5O3
Molecular Weight 461.4882
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EMBUSARTAN

SMILES

CCCCC1=CC(=CC(=O)N1CC2=C(F)C=C(C=C2)C3=C(C=CC=C3)C4=NN=NN4)C(=O)OC

InChI

InChIKey=LYVGOAYMIAQLHI-UHFFFAOYSA-N
InChI=1S/C25H24FN5O3/c1-3-4-7-19-12-18(25(33)34-2)14-23(32)31(19)15-17-11-10-16(13-22(17)26)20-8-5-6-9-21(20)24-27-29-30-28-24/h5-6,8-14H,3-4,7,15H2,1-2H3,(H,27,28,29,30)

HIDE SMILES / InChI
Embusartan or BAY106734 (6-n-butyl-4-methoxycarbonyl-2-oxo-1[(2'-(1H-tetrazol-5-yl) -3-fluorobiphenyl-4-yl)methyl] 1,2-dihydropyridine) is an angiotensin II receptors antagonist. Embusartan has beneficial effects in different animal hypertension models. Embusartan appears as a potent and specific new inhibitor of angiotensin II-induced growth-related events in vascular smooth muscle cells. It was being developed for the treatment of hypertension.

CNS Activity

Curator's Comment: Embusartan is CNS penetrant and active in animals. No human data available.

Approval Year

PubMed

PubMed

TitleDatePubMed
Long-term blockade of the angiotensin II receptor in renin transgenic rats, salt-loaded Dahl rats, and stroke-prone spontaneously hypertensive rats.
1997 Sep
Effects of BAY 10-6734 (Embusartan), a new angiotensin II type I receptor antagonist, on vascular smooth muscle cell growth.
1999 Apr
AT(1) receptor blockers prevent sympathetic hyperactivity and hypertension by chronic ouabain and hypertonic saline.
2001 Mar
Patents

Patents

Sample Use Guides

24 healthy male volunteers received single oral doses of 20-300 mg BAY 10-6734.
Route of Administration: Oral
Name Type Language
EMBUSARTAN
INN   WHO-DD  
INN  
Official Name English
Embusartan [WHO-DD]
Common Name English
embusartan [INN]
Common Name English
METHYL 6-BUTYL-1-(2-FLUORO-4-(O-1H-TETRAZOL-5-YLPHENYL)BENZYL)-1,2-DIHYDRO-2-OXOISONICOTINATE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C66930
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL1742441
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
PRIMARY
PUBCHEM
133000
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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EPA CompTox
DTXSID50166029
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
PRIMARY
NCI_THESAURUS
C81521
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
PRIMARY
MESH
C109119
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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CAS
156001-18-2
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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SMS_ID
100000080754
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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EVMPD
SUB06501MIG
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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INN
7527
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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FDA UNII
4MY73645XA
Created by admin on Fri Dec 15 15:35:45 GMT 2023 , Edited by admin on Fri Dec 15 15:35:45 GMT 2023
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