2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE) Endogenous Metabolite
  4. Vardenafil hydrochloride

Vardenafil hydrochloride 

Cat. No.: HY-B0442A Purity: 99.48%
COA Handling Instructions

Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride 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 Chemical Structure

Vardenafil hydrochloride Chemical Structure

CAS No. : 224785-91-5

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Based on 2 publication(s) in Google Scholar

Other Forms of Vardenafil hydrochloride:

Vardenafil hydrochloride Related Antibodies

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Description

Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride 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 competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].

IC50 & Target[2]

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Vardenafil hydrochloride Related Antibodies
In Vivo

Vardenafil hydrochloride (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury[4].
? Vardenafil hydrochloride (I.V.; 0.17 mg/kg once daily; 7 days) protects liver against Con A–induced hepatitis, and decreases the expression of NF-[5].
? Vardenafil hydrochloride (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].

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

525.06

Appearance

Solid

Formula

C23H33ClN6O4S
CAS No.
SMILES

CCCC1=NC(C)=C2N1N=C(C(C=C(S(=O)(N3CCN(CC)CC3)=O)C=C4)=C4OCC)NC2=O.Cl
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: 

DMSO : 100 mg/mL (190.45 mM; Need ultrasonic)

H2O : ≥ 100 mg/mL (190.45 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 120 mg/mL (228.55 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Vardenafil hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Vardenafil224785-91-5Phosphodiesterase (PDE)Endogenous MetabolitecGMPselectivesmoothmuscleNOstimulationerectiledysfunctionimpotencepharmacokineticserectile dysfunctionhepatitisZucker diabetic fatty (ZDF) ratsdiabetesInhibitorinhibitorinhibit

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