Vardenafil
Based on 6 publication(s) in Google Scholar
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 224785-90-4
- Formula: C23H32N6O4S
- Molecular Weight:488.60
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vardenafil
MoreAll Endogenous Metabolite Isoforms
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Biological Activity
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PDE5 0.7 nM (IC50) |
PDE6 11 nM (IC50) |
PDE1 180 nM (IC50) |
PDE3 >1000 nM (IC50) |
PDE4 >1000 nM (IC50) |
Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM[1].
Vardenafil increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vardenafil (I.V.; 0.17 mg/kg once daily; 7 days) protects liver against Con A–induced hepatitis, and decreases the expression of NF-??B and iNOS in hepatic tissue[5].
Vardenafil (P.O.; 10 mg/kg once daily; 25 weeks) prevents the reduction of tissue cGMP levels and the increase in 3-NT generation in ZDF hearts[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury[4]
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Dosage:0.03 mg/kg
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Administration:Intravenous injection
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Result:Restored normal erectile responses with a combind administration of BAY 60-4552 (0.03, 0.3 mg/kg).
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Animal Model:Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g)[5]
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Dosage:0.17 mg/kg
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Administration:Intravenous injection; once daily, for 7 days; as a pretreatment
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Result:Reduced the levels of serum transaminases and alleviated Con A-induced hepatitis.
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Animal Model:Male 7-week-old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)[6]
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Dosage:10 mg/kg
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Administration:Oral gavage; once daily, for 25 weeks
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Result:Improved myofilament function in diabetic rat hearts.
Chemical Information
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CAS No. 224785-90-4
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Appearance Solid
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Molecular Weight 488.60
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Formula C23H32N6O4S
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Color White to off-white
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SMILES
CCCC1=NC(C)=C2N1N=C(C(C=C(S(=O)(N3CCN(CC)CC3)=O)C=C4)=C4OCC)NC2=O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (6)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Life Sci
The PDE5 inhibitor, vardenafil, ameliorates progressive pathological changes in a focal segmental glomerulosclerosis mouse model. [Abstract]2022 Nov 15:309:120992. PMID: 36155178 -
Analyst
Evaluation of vardenafil's metabolic stability in human liver microsomes through ultra-fast UPLC-MS/MS for quantitative analysis, including assessments of greenness, ADME properties, DEREK alerts, and metabolic lability. [Abstract]2026 Jun 15;151(12):3550-3561. PMID: 42132584 -
Anim Cells Syst (Seoul)
Pharmacokinetic, metabolic stability, plasma protein binding and CYP450s inhibition/induction assessment studies of N-(2-pyridylmethyl)-2-hydroxiymethyl-1-pyrrolidinyl-4-(3-chloro-4-methoxy-benzylamino)-5-pyrimidine-carboxamide as potential type 5 phosphodiesterase inhibitors. [Abstract]2019 May 16;23(3):155-163. PMID: 31231578 -
Solvent & Solubility
DMSO : 25 mg/mL (51.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (728 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[5]. Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31(3). [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0467 mL | 10.2333 mL | 20.4666 mL | 51.1666 mL |
| 5 mM | 0.4093 mL | 2.0467 mL | 4.0933 mL | 10.2333 mL | |
| 10 mM | 0.2047 mL | 1.0233 mL | 2.0467 mL | 5.1167 mL | |
| 15 mM | 0.1364 mL | 0.6822 mL | 1.3644 mL | 3.4111 mL | |
| 20 mM | 0.1023 mL | 0.5117 mL | 1.0233 mL | 2.5583 mL | |
| 25 mM | 0.0819 mL | 0.4093 mL | 0.8187 mL | 2.0467 mL | |
| 30 mM | 0.0682 mL | 0.3411 mL | 0.6822 mL | 1.7056 mL | |
| 40 mM | 0.0512 mL | 0.2558 mL | 0.5117 mL | 1.2792 mL | |
| 50 mM | 0.0409 mL | 0.2047 mL | 0.4093 mL | 1.0233 mL |
Vardenafil Related Classifications
HY-B0442 Related Classifications
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