Sildenafil citrate

SKU: orb1310584

Description

Sildenafil citrate (UK-92480 citrate) is a selective PDE5 inhibitor that elevates cGMP levels. It is widely employed in erectile dysfunction research and clinically for pulmonary arterial hypertension. This compound is a crucial tool for investigating cGMP signaling pathways in both in vitro enzymatic assays and in vivo vascular studies.

Research Area

Neuroscience

Key Properties

• CAS Number: 171599-83-0
• MW: 666.7
• Purity: >98%
• Formula: C₂₂H₃₀N₆O₄S C₆H₈O₇
• SMILES: OC(=O)CC(O)(CC(O)=O)C(O)=O.CCCC1=NN(C)C2=C1N=C(NC2=O)C1=CC(=CC=C1OCC)S(=O)(=O)N1CCN(C)CC1
• Target: PDE (Phosphodiesterase)
• Solubility: Soluble in DMSO (up to 60 mg/ml).

Bioactivity

• Target IC50:
  PDE6:33 nM|PDE5:3.5 nM
• In Vivo:
  Within anesthetized canines, Sildenafil citrate enhances erectile function of the penis following pelvic nerve stimulation. In Sprague-Dawley rats, daily administration of Sildenafil (20 mg/kg) improves erectile function in a time- and dose-dependent manner, while concurrently reducing the apoptosis index significantly and increasing the phosphorylation of akt and eNOS.
• In Vitro:
  In endothelial cells, Sildenafil enhances insulin signaling and nitric oxide (NO) production by mitigating oxidative stress induced by hyperglycemia and elevating intracellular calcium levels (Ca2+). Sildenafil citrate acts as a potent, reversible, selective inhibitor of phosphodiesterase type 5 (PDE5), effectively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP) with an inhibition constant (Ki) of approximately 3 nM.
• Cell Research:
  Sildenafil is prepared in DMSO and stored, and then diluted with appropriate medium before use. Cells at approximately 90% confluence are harvested with 0.1% trypsin/0.01% ethylene diamine tetraacetic acid (EDTA) solution and seeded into a 96-well plate at a density of 2×104 cells/well and grown in RPMI-1640 containing 10% FBS for three days, followed by serum starvation for three days. Cells are then incubated for different time with various concentration of serotonin or 1 μM Sildenafil followed by serotonin with or without U0126, as indicated. Control cells are treated in the same way except sterile PBS replaced the drug. After treatment, medium is changed to fresh medium, and cells are incubated with 5 g/L of MTT for four hours. MTT is then dissolved with 150 μL of 10% DMSO for 20 minutes. The optical densities (OD) in the 96-well plates are determined using a microplate reader at 570 nm.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UK-92480

Compound Identifiers

PubChem CID

135413523