1. Vardenafil hydrochloride trihydrate

Vardenafil hydrochloride trihydrate 

Cat. No.: HY-B0442B Purity: 99.67%
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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

Vardenafil hydrochloride trihydrate Chemical Structure

CAS No. : 330808-88-3

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Based on 1 publication(s) in Google Scholar

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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

IC50: 0.7 nM (PDE5); 180 nM (PDE1); 11 nM (PDE6); >1000 nM (PDE3, PDE4)[1]

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-𝜅B 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.
Molecular Weight

579.11

Formula

C23H39ClN6O7S

CAS No.
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

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)

Purity & Documentation

Purity: 99.67%

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Vardenafil hydrochloride trihydrate
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