Vardenafil dihydrochloride
Based on 6 publication(s) in Google Scholar
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-.
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- CAS. Nr.: 224789-15-5
- Formel: C23H34Cl2N6O4S
- Molecular Weight:561.52
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Vardenafil dihydrochloride
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Biologische Aktivität
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PDE5 0.7 nM (IC50) |
PDE1 180 nM (IC50) |
PDE6 11 nM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
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. Nr. 224789-15-5
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Molecular Weight 561.52
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Formel C23H34Cl2N6O4S
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SMILES
O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.[H]Cl.[H]Cl
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
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 -
Reinheit & Dokumentation
Verweise
[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]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Vardenafil dihydrochloride Related Classifications
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