| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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Description: Vardenafil HCl, also known as BAY 38-9456 HCl, is a novel and potent PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil is 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. Vardenafil's indications and contraindications are the same as with other PDE5 inhibitors; it is closely related in function to sildenafil citrate (Viagra) and tadalafil (Cialis). The difference between the vardenafil molecule and sildenafil citrate is a nitrogen atom's position and the change of sildenafil's piperazine ring methyl group to an ethyl group. Tadalafil is structurally different from both sildenafil and vardenafil. Vardenafil's relatively short effective time is comparable to but somewhat longer than sildenafil's.
| ln Vitro |
Vardenafil hydrochloride has an IC50 of 0.7 nM, which selectively prevents PDE5 from hydrolyzing cGMP[1]. The body's sinuses enlarge and blood flow is enhanced when vardenafil hydrochloride raises intracellular cGMP levels in the corpus cavernosum tissue of the penis [3].
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| ln Vivo |
In rats suffering from cavernous nerve damage, vardenafil hydrochloride (IV; 0.03 mg/kg) exerts a promoting effect [4]. Vardenafil hydrochloride (IV; once daily; 0.17 mg/kg; 7 days) lowers NF- in liver tissue and shields the liver from hepatitis caused by Con A [5]. In ZDF hearts, vardenafil hydrochloride (oral; 10 mg/kg once daily; 25 weeks) inhibits both the rise in 3-NT synthesis and the fall in tissue cGMP levels [6].
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| 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 combind 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. |
| Molecular Formula |
C23H32N6O4S.HCL
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|---|---|
| Molecular Weight |
525.06
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| CAS # |
224785-91-5
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| Related CAS # |
Vardenafil;224785-90-4;Vardenafil hydrochloride trihydrate;330808-88-3;Vardenafil dihydrochloride;224789-15-5
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| SMILES |
CCCC1=NC(C)=C2N1N=C(C(C=C(S(=O)(N3CCN(CC)CC3)=O)C=C4)=C4OCC)NC2=O.Cl
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~190.45 mM)
H2O : ≥ 100 mg/mL (~190.45 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (228.55 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9045 mL | 9.5227 mL | 19.0454 mL | |
| 5 mM | 0.3809 mL | 1.9045 mL | 3.8091 mL | |
| 10 mM | 0.1905 mL | 0.9523 mL | 1.9045 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.
Calculation results
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.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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