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PF-00489791

Catalog No. T28360 CAS 853003-48-2

Synonyms: PF-4634817, PF 4634817, PF00489791, PF 00489791, PF4634817

PF-00489791 (PF4634817) is a long-acting PDE5 inhibitor with hypotensive activity for the study of diabetic nephropathy.

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PF-00489791, CAS 853003-48-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 105.00
5 mg	In stock	$ 228.00
10 mg	In stock	$ 347.00
25 mg	In stock	$ 578.00
50 mg	In stock	$ 825.00

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Purity: 100%

Biological Description

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Description

PF-00489791 (PF4634817) is a long-acting PDE5 inhibitor with hypotensive activity for the study of diabetic nephropathy.

In vivo

The novel, highly specific, and long-acting PDE5 inhibitor, PF-00489791, was assessed in a multinational, multicenter, randomized, double-blind, placebo-controlled, parallel-group trial of subjects with type 2 diabetes mellitus and overt nephropathy receiving angiotensin-converting enzyme inhibitor or angiotensin receptor blocker background therapy. In total, 256 subjects with an eGFR between 25 and 60 ml/min per 1.73 m2 and macroalbuminuria defined by a urinary albumin-to-creatinine ratio >300 mg/g, were randomly assigned 3:1, respectively, to receive PF-00489791 (20 mg) or placebo orally, once daily for 12 weeks. Using the predefined primary assessment of efficacy (Bayesian analysis with informative prior), we observed a significant reduction in the urinary albumin-to-creatinine ratio of 15.7% (ratio 0.843; 95% credible interval 0.73 to 0.98) in response to the 12-week treatment with PF-00489791 compared with placebo. PF-00489791 was safe and generally well tolerated in this patient population. Most common adverse events were mild in severity and included headache and upper gastrointestinal events. In conclusion, the safety and efficacy profile of PDE5 inhibitor PF-00489791 supports further investigation as a novel therapy to improve renal outcomes in DN.[1]

Synonyms	PF-4634817, PF 4634817, PF00489791, PF 00489791, PF4634817
Molecular Weight	476.55
Formula	C20H28N8O4S
CAS No.	853003-48-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Scheele W, Diamond S, Gale J, Clerin V, Tamimi N, Le V, Walley R, Grover-Páez F, Perros-Huguet C, Rolph T, El Nahas M. Phosphodiesterase Type 5 Inhibition Reduces Albuminuria in Subjects with Overt Diabetic Nephropathy. J Am Soc Nephrol. 2016 Apr 25. pii: ASN.2015050473. [Epub ahead of print] PubMed PMID: 27113485. 2. Afsar B, et al. Phosphodiesterase type 5 inhibitors and kidney disease. Int Urol Nephrol. 2015 Sep;47(9):1521-8. 3. Wolk R, et al. Blood pressure lowering effects of a new long-acting inhibitor of phosphodiesterase 5 in patients with mild to moderate hypertension. Hypertension. 2009 Jun;53(6):1091-7.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

PF-00489791 853003-48-2 Metabolism PDE PF-4634817 PF 4634817 PF00489791 PF 00489791 PF4634817 inhibitor inhibit

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