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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
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.

Approval Year

PubMed

PubMed

TitleDatePubMed
Blood pressure lowering effects of a new long-acting inhibitor of phosphodiesterase 5 in patients with mild to moderate hypertension.
2009 Jun
Phosphodiesterase type 5 inhibitors and kidney disease.
2015 Sep
Phosphodiesterase Type 5 Inhibition Reduces Albuminuria in Subjects with Overt Diabetic Nephropathy.
2016 Nov
Patents

Sample Use Guides

20 mg daily for 12 weeks
Route of Administration: Oral
Name Type Language
PF-00489791
Common Name English
1H-PYRAZOLO(4,3-D)PYRIMIDINE-3-CARBOXAMIDE, 1-(2-ETHOXYETHYL)-5-(ETHYLMETHYLAMINO)-7-((4-METHYL-2-PYRIDINYL)AMINO)-N-(METHYLSULFONYL)
Systematic Name English
PF-489,791
Code English
UK-489,791
Code English
Code System Code Type Description
FDA UNII
2S27T3DSZ3
Created by admin on Fri Dec 15 19:48:05 GMT 2023 , Edited by admin on Fri Dec 15 19:48:05 GMT 2023
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DRUG BANK
DB11736
Created by admin on Fri Dec 15 19:48:05 GMT 2023 , Edited by admin on Fri Dec 15 19:48:05 GMT 2023
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SMS_ID
300000041311
Created by admin on Fri Dec 15 19:48:05 GMT 2023 , Edited by admin on Fri Dec 15 19:48:05 GMT 2023
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CAS
853003-48-2
Created by admin on Fri Dec 15 19:48:05 GMT 2023 , Edited by admin on Fri Dec 15 19:48:05 GMT 2023
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PUBCHEM
11465695
Created by admin on Fri Dec 15 19:48:05 GMT 2023 , Edited by admin on Fri Dec 15 19:48:05 GMT 2023
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