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Details

Stereochemistry ACHIRAL
Molecular Formula C23H21N7O
Molecular Weight 411.4591
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TASOSARTAN

SMILES

CC1=NC2=C(CCC(=O)N2CC3=CC=C(C=C3)C4=C(C=CC=C4)C5=NN=NN5)C(C)=N1

InChI

InChIKey=ADXGNEYLLLSOAR-UHFFFAOYSA-N
InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)

HIDE SMILES / InChI

Molecular Formula C23H21N7O
Molecular Weight 411.4591
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Tasosartan is infrequently in the treatment of hypertension and heart failure. The manufacturer withdrew it from FDA review after phase III clinical trials showed elevated transaminases. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance.

Originator

Curator's Comment: # Wyeth-Ayerst (American Home Products)

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding.
2000 Nov
Pharmacology of AT1-receptor blockers.
2001
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.
2002 Aug 5
Patents

Sample Use Guides

Single doses of tasosartan (100 mg p.o. and 50 mg i.v) was compared in 12 healthy subjects in a randomized, double blind studies.
Route of Administration: Other
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Fri Dec 15 17:58:19 GMT 2023
Edited
by admin
on Fri Dec 15 17:58:19 GMT 2023
Record UNII
48G92V856H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TASOSARTAN
INN   MART.   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
TASOSARTAN [MI]
Common Name English
Tasosartan [WHO-DD]
Common Name English
WAY-ANA-756
Code English
TASOSARTAN [USAN]
Common Name English
tasosartan [INN]
Common Name English
TASOSARTAN [MART.]
Common Name English
ANA-756
Code English
5,8-DIHYDRO-2,4-DIMETHYL-8-((2'-(1H-TETRAZOL-5-YL)(1,1'-BIPHENYL)-4-YL)METHYL)PYRIDO(2,3-D)PYRIMIDIN-7(6H)-ONE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C66930
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
WHO-VATC QC09CA05
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
WHO-ATC C09CA05
Created by admin on Fri Dec 15 17:58:19 GMT 2023 , Edited by admin on Fri Dec 15 17:58:19 GMT 2023
Code System Code Type Description
WIKIPEDIA
TASOSARTAN
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
EPA CompTox
DTXSID40163148
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
FDA UNII
48G92V856H
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
DRUG CENTRAL
3839
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
EVMPD
SUB10834MIG
Created by admin on Fri Dec 15 17:58:19 GMT 2023 , Edited by admin on Fri Dec 15 17:58:19 GMT 2023
PRIMARY
PUBCHEM
60919
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
CAS
145733-36-4
Created by admin on Fri Dec 15 17:58:19 GMT 2023 , Edited by admin on Fri Dec 15 17:58:19 GMT 2023
PRIMARY
DRUG BANK
DB01349
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
SMS_ID
100000082406
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
ChEMBL
CHEMBL432162
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
INN
7334
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
NCI_THESAURUS
C152517
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
MERCK INDEX
m951
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY Merck Index
MESH
C086167
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
USAN
GG-31
Created by admin on Fri Dec 15 17:58:20 GMT 2023 , Edited by admin on Fri Dec 15 17:58:20 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
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METABOLITE ACTIVE -> PARENT
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ACTIVE MOIETY