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
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)
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
Title | Date | PubMed |
---|---|---|
Blood pressure lowering effects of a new long-acting inhibitor of phosphodiesterase 5 in patients with mild to moderate hypertension. | 2009 Jun |
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Phosphodiesterase type 5 inhibitors and kidney disease. | 2015 Sep |
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Phosphodiesterase Type 5 Inhibition Reduces Albuminuria in Subjects with Overt Diabetic Nephropathy. | 2016 Nov |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27113485
20 mg daily for 12 weeks
Route of Administration:
Oral
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2S27T3DSZ3
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DB11736
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300000041311
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853003-48-2
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11465695
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ACTIVE MOIETY