Vardenafil HCl Trihydrate

Alias: BAY38-9456; BAY 38-9456; BAY-38-9456; trade names: Levitra; Staxyn; Vivanza; Vardenafil hydrochloride trihydrate; Vardenafil HCl; Levitra; Staxyn; Vivanza
Cat No.:V0781 Purity: ≥98%
Vardenafil HCl Trihydrate (formerly also known as BAY 38-9456, trade names Levitra; Staxyn; Vivanza) is an approved medication acting as aphosphodiesterase/PDE inhibitor with important biological activity.
Vardenafil HCl Trihydrate Chemical Structure CAS No.: 330808-88-3
Product category: PDE
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
Other Sizes

Other Forms of Vardenafil HCl Trihydrate:

  • Vardenafil HCl
  • Vardenafil 2HCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Description: Vardenafil HCl Trihydrate (formerly also known as BAY 38-9456, trade names Levitra; Staxyn; Vivanza) is an approved medication acting as a phosphodiesterase/PDE inhibitor with important biological activity. It inhibits PDE5 and PDE1 with IC50s of 0.7 and 180 nM, respectively. Vardenafil has been approved used for treating erectile dysfunction. Vardenafil (VAR) is synthetic, highly selective, and potent inhibitor of phosphodiesterase-5 which competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Vardenafil hydrochloride trihydrate inhibits PDE5-mediated cGMP hydrolysis with an IC50 of 0.7 nM[1]. Vardenafil hydrochloride trihydrate raises intracellular cGMP levels in the penis' cavernosum tissue, causing sinus dilation and increased blood flow [3].
ln Vivo
In rats suffering from cavernous nerve damage, vardenafil hydrochloride trihydrate (IV; 0.03 mg/kg) shows facilitative effects[4]. Vardenafil hydrochloride trihydrate (IV; 0.17 mg/kg once daily; 7 days) reduces the expression of iNOS and NF-���B in hepatic tissue and shields the liver from Con A-induced hepatitis[5]. In ZDF hearts, vardenafil hydrochloride trihydrate (PO; 10 mg/kg once daily; 25 weeks) inhibits both the rise in 3-NT production and the decrease in tissue cGMP levels [6].
Animal Protocol
Animal/Disease Models: Male rat (9weeks old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury[4]
Doses: 0.03 mg/kg
Route of Administration: intravenous (iv) injection
Experimental Results: Restored normal erectile responses with a combined administration of BAY 60-4552 (0.03, 0.3 mg/kg).

Animal/Disease Models: Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g)[5]
Doses: 0.17 mg/kg
Route of Administration: intravenous (iv) injection; one time/day, for 7 days; as a pretreatment
Experimental Results: decreased the levels of serum transaminases and alleviated Con A-induced hepatitis.

Animal/Disease Models: Male 7weeks old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)[6]
Doses: 10 mg/kg
Route of Administration: po (oral gavage); one time/day, for 25 weeks
Experimental Results: Improved myofilament function in diabetic rat hearts.
References
[1]. Saenz de Tejada I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001;13(5):282-290.
[2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.
[3]. Gresser U, et al. Erectile dysfunction: comparison of efficacy and side effects of the PDE-5 inhibitors sildenafil, vardenafil and tadalafil--review of the literature. Eur J Med Res. 2002 Oct 29. 7(10):435-46.
[4]. Oudot A, et al. Combination of BAY 60-4552 and vardenafil exerts proerectile facilitator effects in rats with cavernous nerve injury: a proof of concept study for the treatment of phosphodiesterase type 5 inhibitor failure. Eur Urol. 2011 Nov. 60(5):1020-6.
[5]. Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31(3).
[6]. Bódi B, et al. Long-Term PDE-5A Inhibition Improves Myofilament Function in Left and Right Ventricular Cardiomyocytes through Partially Different Mechanisms in Diabetic Rat Hearts. Antioxidants (Basel). 2021 Nov 6. 10(11):1776.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H32N6O4S.HCL.3H2O
Molecular Weight
579.11
CAS #
330808-88-3
SMILES
O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.[H]Cl.[H]Cl.[H]O[H].[H]O[H].[H]O[H]
InChi Key
NEAUGLIJDBPHAY-UHFFFAOYSA-N
Chemical Name
2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one dihydrochloride trihydrate
Synonyms
BAY38-9456; BAY 38-9456; BAY-38-9456; trade names: Levitra; Staxyn; Vivanza; Vardenafil hydrochloride trihydrate; Vardenafil HCl; Levitra; Staxyn; Vivanza
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 116 mg/mL (200.3 mM)
Water:116 mg/mL (200.3 mM)
Ethanol: 20 mg/mL (34.53 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7268 mL 8.6339 mL 17.2679 mL
5 mM 0.3454 mL 1.7268 mL 3.4536 mL
10 mM 0.1727 mL 0.8634 mL 1.7268 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data

  • Vardenafil HCl Trihydrate
    Potency of inhibition of PDE catalytic activity by PDE5 inhibitors.




    Vardenafil HCl Trihydrate


    Affinity of PDE5 for binding 3H inhibitors.Mol Pharmacol.2004 Jul;66(1):144-52.
  • Vardenafil HCl Trihydrate

    Effects of nucleotides and inhibitors on binding of 3H inhibitors to PDE5.Mol Pharmacol.2004 Jul;66(1):144-52.


    Vardenafil HCl Trihydrate

    Effect of cGMP on [3H]vardenafil binding at 4° and 30°C.Mol Pharmacol.2004;66(1):144-52.


  • Vardenafil HCl Trihydrate

    Dissociation of 3H inhibitors from PDE5 after infinite dilution.Mol Pharmacol.2004 Jul;66(1):144-52.
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