U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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

Molecular Formula C25H24FN5O3
Molecular Weight 461.4882
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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
Substance Class Chemical
Created
by admin
on Fri Dec 15 15:35:45 UTC 2023
Edited
by admin
on Fri Dec 15 15:35:45 UTC 2023
Record UNII
4MY73645XA
Record Status Validated (UNII)
Record Version
  • Download
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 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
Code System Code Type Description
ChEMBL
CHEMBL1742441
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
PUBCHEM
133000
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
EPA CompTox
DTXSID50166029
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
NCI_THESAURUS
C81521
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
MESH
C109119
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
CAS
156001-18-2
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
SMS_ID
100000080754
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
EVMPD
SUB06501MIG
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
INN
7527
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
FDA UNII
4MY73645XA
Created by admin on Fri Dec 15 15:35:45 UTC 2023 , Edited by admin on Fri Dec 15 15:35:45 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY