1. Metabolic Enzyme/Protease
  2. Endogenous Metabolite
    Phosphodiesterase (PDE)
  3. Vardenafil dihydrochloride

Vardenafil dihydrochloride 

Cat. No.: HY-B0442C
Handling Instructions

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

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

Vardenafil dihydrochloride Chemical Structure

Vardenafil dihydrochloride Chemical Structure

CAS No. : 224789-15-5

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Description

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

IC50 & Target

PDE5

0.7 nM (IC50)

PDE1

180 nM (IC50)

PDE6

11 nM (IC50)

In Vitro

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

In Vivo

Vardenafil dihydrochloride (0.03 mg/kg; i.v.) exhibits facilitator effects in rats with cavernous nerve injury[4].
Vardenafil dihydrochloride (0.17 mg/kg; i.v.; once daily; 7 d) protects liver against Con A–induced hepatitis, and decreases the expression of NF-𝜅B and iNOS in hepatic tissue[5].
Vardenafil dihydrochloride (10 mg/kg; p.o.; 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.
Molecular Weight

561.52

Formula

C23H34Cl2N6O4S

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Vardenafil dihydrochloride
Cat. No.:
HY-B0442C
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