Vardenafil hydrochloride trihydrate

Name: Vardenafil hydrochloride trihydrate
Brand: MedChemExpress
SKU: HY-B0442B
Rating: 5.0 (4 reviews)

Cat. No.: HY-B0442B Purity: 99.67%: Data Sheet
COA

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Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

For research use only. We do not sell to patients.

Vardenafil hydrochloride trihydrate Chemical Structure

CAS No. : 330808-88-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	Get quote
1 g	Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Vardenafil hydrochloride trihydrate:

Vardenafil In-stock
Vardenafil hydrochloride In-stock
Vardenafil dihydrochloride Get quote
Vardenafil hydrochloride trihydrate (Standard) Get quote

4 Publications Citing Use of MCE Vardenafil hydrochloride trihydrate

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Purity & Documentation
References
Customer Review

Description

Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4^[1]. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels^[2]. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

IC₅₀ & Target

PDE5

0.7 nM (IC₅₀)

PDE6

11 nM (IC₅₀)

PDE1

180 nM (IC₅₀)

PDE3

>1000 nM (IC₅₀)

PDE4

>1000 nM (IC₅₀)

In Vitro

Vardenafil hydrochloride trihydrate specifically inhibits the hydrolysis of cGMP by PDE5 with an IC₅₀ of 0.7 nM^[1].
Vardenafil hydrochloride trihydrate 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.

In Vivo

Vardenafil hydrochloride trihydrate (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury^[4].
Vardenafil hydrochloride trihydrate (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 hydrochloride trihydrate (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.

Animal Model:	Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury^[4]
Dosage:	0.03 mg/kg
Administration:	Intravenous injection
Result:	Restored normal erectile responses with a combind administration of BAY 60-4552 (0.03, 0.3 mg/kg).

Animal Model:	Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g)^[5]
Dosage:	0.17 mg/kg
Administration:	Intravenous injection; once daily, for 7 days; as a pretreatment
Result:	Reduced the levels of serum transaminases and alleviated Con A-induced hepatitis.

Animal Model:	Male 7-week-old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)^[6]
Dosage:	10 mg/kg
Administration:	Oral gavage; once daily, for 25 weeks
Result:	Improved myofilament function in diabetic rat hearts.

Clinical Trial

Molecular Weight

579.11

Formula

C₂₃H₃₉ClN₆O₇S

CAS No.

330808-88-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.Cl.O.O.O

Structure Classification

Others

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (172.68 mM)

DMSO : 25 mg/mL (43.17 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.32 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.32 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.67%

Select Batch:

Data Sheet (283 KB) SDS (644 KB)

COA (254 KB) LCMS (108 KB)

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	1.7268 mL	8.6339 mL	17.2679 mL	43.1697 mL
	5 mM	0.3454 mL	1.7268 mL	3.4536 mL	8.6339 mL
	10 mM	0.1727 mL	0.8634 mL	1.7268 mL	4.3170 mL
	15 mM	0.1151 mL	0.5756 mL	1.1512 mL	2.8780 mL
	20 mM	0.0863 mL	0.4317 mL	0.8634 mL	2.1585 mL
	25 mM	0.0691 mL	0.3454 mL	0.6907 mL	1.7268 mL
	30 mM	0.0576 mL	0.2878 mL	0.5756 mL	1.4390 mL
	40 mM	0.0432 mL	0.2158 mL	0.4317 mL	1.0792 mL
H₂O	50 mM	0.0345 mL	0.1727 mL	0.3454 mL	0.8634 mL
	60 mM	0.0288 mL	0.1439 mL	0.2878 mL	0.7195 mL
	80 mM	0.0216 mL	0.1079 mL	0.2158 mL	0.5396 mL
	100 mM	0.0173 mL	0.0863 mL	0.1727 mL	0.4317 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.