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

Details

Stereochemistry ACHIRAL
Molecular Formula C20H28N8O4S
Molecular Weight 476.553
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-00489791

SMILES

CCOCCN1N=C(C(=O)NS(C)(=O)=O)C2=C1C(NC3=NC=CC(C)=C3)=NC(=N2)N(C)CC

InChI

InChIKey=ZUHZNKJIJDAJFD-UHFFFAOYSA-N
InChI=1S/C20H28N8O4S/c1-6-27(4)20-23-15-16(19(29)26-33(5,30)31)25-28(10-11-32-7-2)17(15)18(24-20)22-14-12-13(3)8-9-21-14/h8-9,12H,6-7,10-11H2,1-5H3,(H,26,29)(H,21,22,23,24)

HIDE SMILES / InChI

Molecular Formula C20H28N8O4S
Molecular Weight 476.553
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

PF-00489791 is the novel, selective and long-acting phosphodiesterase type 5 (PDE5) inhibitor. PF-00489791 was safe and generally well tolerated in overt diabetic nephropathy patient population. Most common adverse events were mild in severity and included headache and upper gastrointestinal events. PF-00489791 is the first long-acting PDE5 inhibitor to demonstrate significant reduction of albuminuria when added to standard of care therapy in subjects with type 2 diabetes mellitus and overt diabetic nephropathy. In addition, PF-00489791 causes a clinically meaningful and sustained blood pressure lowering in patients with hypertension.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
20 mg daily for 12 weeks
Route of Administration: Oral
Substance Class Chemical
Record UNII
2S27T3DSZ3
Record Status Validated (UNII)
Record Version