A PDE5 inhibitor (IC50s = 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum

Sildenafil Citrate – 10 mg

Brand:
Cayman
CAS:
171599-83-0
Storage:
-20
UN-No:
Non-Hazardous - /

Sildenafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with IC50 values of 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively.{21636} It is selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively). Sildenafil reverses glucose-induced decreases in angiopoietin 1 (ANG1) expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro and increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy.{42390} It increases the ratio of maximum intracavernosal pressure to mean arterial blood pressure (ICP/MAP), a measure of erectile function, in castrated rats when administered at a dose of 20 mg/kg per day.{42389} Sildenafil (0.5 mg/kg) also reduces cardiac arrest and resuscitation-induced increases in angiotensin II (Item No. 17150), angiotensin converting enzyme (ACE), ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury.{42391} Formulations containing sildenafil have been used in the treatment of erectile dysfunction, pulmonary arterial hypertension, and high-altitude pulmonary edema associated with altitude sickness.  

 

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Description

A PDE5 inhibitor (IC50s = 3.6 and 3 nM for PDE5 activity in isolated rabbit platelets and human corpus cavernosum, respectively); selective for PDE5 over PDE1 and PDE3 (IC50s = 0.26 and 65 μM, respectively); reverses glucose-induced decreases in ANG1 expression and reduction of capillary-like tube formation by mouse dermal endothelial cells in vitro; increases the number of functional blood vessels and regional blood flow in the sciatic nerve in a db/db mouse model of diabetic peripheral neuropathy; increases ICP/MAP ratio in castrated rats at 20 mg/kg per day; reduces cardiac arrest and resuscitation-induced increases in angiotensin II ACE, ACE2, and various angiotensin receptors and increases survival in a porcine model of ischemia/reperfusion injury,

Formal name: 5-[2-ethoxy-5-[(4-methyl-1-piperazinyl)sulfonyl]phenyl]-1,6-dihydro-1-methyl-3-propyl-7H-pyrazolo[4,3-d]pyrimidin-7-one, 2-hydroxy-1,2,3-propanetricarboxylate

Synonyms:  Apodefil|Tonafil|UK 92480

Molecular weight: 666.7

CAS: 171599-83-0

Purity: ≥98%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cardiovascular System|Vasculature|Angiogenesis||Research Area|Cell Biology|Cell Signaling|cGMP Signaling

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