| Name | Vardenafil hydrochloride trihydrate |
| Description | Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. |
| In vitro | Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle. |
| In vivo | Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through the opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (5.7 mM), Sonication is recommended.
DMSO : 93 mg/mL (160.59 mM), Sonication is recommended.
H2O : 10 mg/mL (17.27 mM), Sonication is recommended.
Ethanol : 16 mg/mL (27.63 mM), Sonication is recommended.
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| Keywords | Zucker diabetic fatty (ZDF) rats | Vardenafil hydrochloride Trihydrate | Vardenafil hydrochloride | Vardenafil HCl | Vardenafil | stimulation | smooth | selective | Phosphodiesterase (PDE) | pharmacokinetics | PDE5 | PDE1 | muscle | Inhibitor | inhibit | impotence | hepatitis | erectile dysfunction | erectile | Endogenous Metabolite | dysfunction | diabetes | cGMP |
| Inhibitors Related | Sucrose | Aceglutamide | Nicotinamide riboside malate | DL-Lysine | D(+)-Raffinose pentahydrate | Guanidine hydrochloride | Malic acid | Formamide | Glycerol | Thymidine | Corn starch | Gluconate Calcium |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | Drug-induced Liver Injury (DILI) Compound Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | FDA-Approved Drug Library | Metabolism Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Human Metabolite Library |
United States
