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| ln Vitro |
At an IC50 of 0.7 nM, the vadenafil salticide tri Hydro selectively prevents PDE5 from hydrolyzing cGMP[1]. The body's sinuses dilate and pump more blood when vardenafil hydrochloride trihydrate is administered because it 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 injury, vardenafil hydrochloride trihydrate (IV; 0.03 mg/kg) has a promoting effect [4]. Vardenafil hydrochloride trihydrate (IV; 0.17 mg/kg once daily; 7 days) lowers the expression of iNOS and NF-���B in liver tissue and shields the liver from hepatitis caused by Con A [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 fall in tissue cGMP levels [6].
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| Animal Protocol |
Animal/Disease Models: Male rats (9 weeks old) underwent laparotomy or bilateral cavernous nerve (CN) crush injury [4]
Doses: 0.03 mg/kg Route of Administration: intravenous (iv) (iv)injection Experimental Results: Combined use of BAY restored normal erectile response 60 -4552 (0.03, 0.3 mg/kg). Animal/Disease Models: Con A-induced liver injury in male Swiss albino mice (20±2g) [5] Doses: 0.17mg/kg Route of Administration: intravenous (iv) (iv)injection; intravenous (iv) (iv)injection. one time/day for 7 days; as a pretreatment Experimental Results:reduces serum aminotransferase levels and reduces Con A-induced hepatitis. Animal/Disease Models: Male 7weeks old Zucker diabetic obese (ZDF) rat (preserved ejection fraction, HFpEF) [6] Doses: 10 mg/kg Route of Administration: po (oral gavage); one time/day for 25 weeks Experimental Results: Improved diabetes Myofilament function in the rat heart. |
| 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.3H2O
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|---|---|
| Molecular Weight |
579.11
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| CAS # |
330808-88-3
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| Related CAS # |
Vardenafil hydrochloride;224785-91-5;Vardenafil dihydrochloride;224789-15-5
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| 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]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| 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.
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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