SAPRISARTAN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H22BrF3N4O4S
Molecular Weight	611.431
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCC1=NC(C2CC2)=C(N1CC3=CC=C4OC(=C(Br)C4=C3)C5=CC=CC=C5NS(=O)(=O)C(F)(F)F)C(N)=O

InChI

InChIKey=DUEWVPTZCSAMNB-UHFFFAOYSA-N

InChI=1S/C25H22BrF3N4O4S/c1-2-19-31-21(14-8-9-14)22(24(30)34)33(19)12-13-7-10-18-16(11-13)20(26)23(37-18)15-5-3-4-6-17(15)32-38(35,36)25(27,28)29/h3-7,10-11,14,32H,2,8-9,12H2,1H3,(H2,30,34)

HIDE SMILES / InChI

Molecular Formula	C25H22BrF3N4O4S
Molecular Weight	611.431
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7932534 | https://adisinsight.springer.com/drugs/800002559

Saprisartan (formerly known as GR 138950) was developed as a potent long-lasting angiotensin II (AT1) receptor antagonist with high oral bioavailability. The drug was used for the treatment of hypertension and heart failure. However, these studies were discontinued.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Type-1 angiotensin II receptor 40 Target ID: P30556 Gene ID: 185.0 Gene Symbol: AGTR1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/7853190	Antagonist 2778

PubMed

Title	Date	PubMed
Bromobenzofuran-based non-peptide antagonists of angiotensin II: GR138950, a potent antihypertensive agent with high oral bioavailability.	1994 Sep 16	7932534
Pharmacological effects of GR138950, a novel angiotensin AT1 receptor antagonist.	1995 Feb	7853190
Investigation of the inhibitory effect of N(G)-nitro-L-arginine methyl ester on the antihypertensive effect of the angiotensin AT1 receptor antagonist, GR138950.	1997 Dec	9421286
The antihypertensive profile of the angiotensin AT1 receptor antagonist, GR138950, and the influence of potential homeostatic compensatory mechanisms in renal hypertensive rats.	1998 Nov	9863652

Patents

Substance Class	Chemical Created by `admin` on `Fri Dec 15 18:52:01 UTC 2023` Edited by `admin` on `Fri Dec 15 18:52:01 UTC 2023`
Record UNII	HS64NG1G69
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SAPRISARTAN

Official Name

English

GR138950

Code

English

saprisartan [INN]

Common Name

English

GR-138950

Code

English

Saprisartan [WHO-DD]

Common Name

English

3-((3-BROMO-2-(2-(TRIFLUOROMETHYLSULFONYLAMINO)PHENYL)-1-BENZOFURAN-5-YL)METHYL)-5-CYCLOPROPYL-2-ETHYLIMIDAZOLE-4-CARBOXAMIDE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66930