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Vardenafil

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Purity:99.88%

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COA HNMR HPLC

Vardenafil

Catalog No. T0096Cas No. 224785-90-4

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

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Pack Size	Price	Availability
25 mg	$31	In Stock
50 mg	$48	In Stock
100 mg	$68	In Stock
500 mg	$162	In Stock
1 g	$238	In Stock
1 mL x 10 mM (in DMSO)	$39	In Stock

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Product Introduction

Bioactivity

Description	Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.
Targets&IC50	PDE5:0.7 nM
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.
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.
Alias	Vivanza, Levitra, Vardenafil hydrochloride

Chemical Properties

Molecular Weight	488.6
Formula	C23H32N6O4S
Cas No.	224785-90-4

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 45 mg/mL (92.1 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0467 mL	10.2333 mL	20.4666 mL	102.3332 mL
5 mM	0.4093 mL	2.0467 mL	4.0933 mL	20.4666 mL
10 mM	0.2047 mL	1.0233 mL	2.0467 mL	10.2333 mL
20 mM	0.1023 mL	0.5117 mL	1.0233 mL	5.1167 mL
50 mM	0.0409 mL	0.2047 mL	0.4093 mL	2.0467 mL

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