product name Vardenafil
Description: Vardenafil, also known as BAY 38-9456, is a novel PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil is used for treating erectile dysfunction. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients.
References: Int J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61.
488.6
Formula
C23H32N6O4S
CAS No.
224785-90-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mM
Water:
Ethanol:
Solubility (In vivo)
Synonyms
BAY38-9456
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). Cell Assay: |
|---|---|
| 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 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 |
| Animal model | Rabbit |
| Formulation & Dosage | 3 mg/kg, p.o. (rabbit) |
| References | Int J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61. |
