Vardenafil

SKU: orb1710756

Description

Vardenafil (Vivanza) is a selective PDE5 inhibitor used for erectile dysfunction research. By blocking cGMP degradation, it enhances the nitric oxide-mediated signaling pathway crucial for penile smooth muscle relaxation. This mechanism is studied in both in vitro enzymatic assays and in vivo models of erectile function.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 224785-90-4
• MW: 488.60
• Purity: 99.64% (May vary between batches)
• Formula: C₂₃H₃₂N₆O₄S
• SMILES: C(CC)C=1N2C(C(=O)N=C(N2)C3=C(OCC)C=CC(S(=O)(=O)N4CCN(CC)CC4)=C3)=C(C)N1
• Target: Endogenous Metabolite,PDE
• Solubility: DMSO:45 mg/mL (92.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.09 mM)

Bioactivity

• Target IC50:
  PDE4:>1000 nM|PDE1:180 nM|PDE5:0.7 nM|PDE3:>1000 nM|PDE6:11 nM
• In Vivo:
  Vardenafil significantly induces relaxation of trabecular smooth muscle elicited by both acetylcholine and electrical stimulation. It competitively inhibits phosphodiesterase type 5 (PDE5), thus enhancing the accumulation and relaxation effect of cyclic guanosine monophosphate (cGMP) in vascular smooth muscle. Its IC50 for specifically inhibiting PDE5-mediated cGMP hydrolysis is 0.7 nM (6.6 nM). At 3 nM (10 nM), Vardenafil notably potentiates the relaxation of human trabecular smooth muscle induced by SNP. At 100 mM, Vardenafil significantly increases cGMP levels in rat hippocampus.
• In Vitro:
  Vardenafil, through the mechanism of mitochondrial K(ATP) channel opening, protects against myocardial ischemia due to reperfusion injury. Oral administration of 3 mg/kg Vardenafil alters object recognition capability in rats. A dose of 30 mg/L orally also upregulates iNOS and proliferating cell nuclear antigen expression (replication of SM cells), leading to the normalization of the rate of dynamic corporal tissue fusion decline and the SM/collagen ratio. Furthermore, Vardenafil induces robust preconditioning-like cardioprotective effects against ischemia/reperfusion injury in rabbits by opening mitochondrial K(ATP) channels. Additionally, it dose-dependently induces an erectile response in rabbits when administered intravenously with Nitroprusside sodium.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Zucker diabetic fatty (ZDF) rats, Vardenafil, Vivanza, stimulation, phosphodiesterase, PED5, cGMP, PDE1, impotence, hepatitis, Levitra, erectile, erectile dysfunction

Compound Identifiers

PubChem CID

135400189