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    Vardenafil HCl Trihydrate
    Vardenafil HCl Trihydrate

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0781
    CAS #: 330808-88-3 Purity ≥98%

    Description: Vardenafil HCl Trihydrate, also known as BAY 38-9456, is a novel PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively. Vardenafil is used for treating erectile dysfunction. Vardenafil (VAR) is synthetic, highly selective, and potent inhibitor of phosphodiesterase-5 which competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients. 

    ReferencesInt J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61.

    Related CAS: 224785-90-4 (free base); 330808-88-3 (HCl trihydrate); 224789-15-5 (2HCl)

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    Molecular Weight (MW)579.11
    FormulaC23H32N6O4S.HCl.3H2O
    CAS No.330808-88-3 (HCl trihydrate); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 116 mg/mL (200.3 mM)
    Water: 116 mg/mL (200.3 mM)
    Ethanol: 20 mg/mL (34.53 mM)
    Other infoChemical Name: 2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one dihydrochloride trihydrate
    InChi Key: NEAUGLIJDBPHAY-UHFFFAOYSA-N
    SMILES Code: O=C1N=C(C2=CC(S(=O)(N3CCN(CC)CC3)=O)=CC=C2OCC)NN4C1=C(C)N=C4CCC.[H]Cl.[H]Cl.[H]O[H].[H]O[H].[H]O[H]
    SynonymsBAY38-9456; BAY 38-9456; BAY-38-9456; trade names: Levitra; Staxyn; Vivanza; Vardenafil hydrochloride trihydrate; Vardenafil HCl; Levitra; Staxyn; Vivanza


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    In Vitro

    In vitro activity: Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.


    Kinase Assay: Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). In contrast, the IC50 of vardenafil for PDE1 was 180 nM; for PDE6, 11 nM; for PDE2, PDE3 and PDE4, more than 1000 nM. Relative to PDE5, the ratios of the IC50 for PDE1 were 257 (60), for PDE6 16 (7.4). 


    Cell Assay: Vardenafil significantly enhanced the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiated both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle.

    In VivoVardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening
    Animal modelRabbit
    Formulation & Dosage3 mg/kg, p.o. (rabbit)
    ReferencesInt J Impot Res. 2001 Oct;13(5):282-90; Neuroscience. 2002;113(2):351-61.


    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Vardenafil HCl Trihydrate
    Potency of inhibition of PDE catalytic activity by PDE5 inhibitors.




    Vardenafil HCl Trihydrate


    Affinity of PDE5 for binding 3H inhibitors.Mol Pharmacol. 2004 Jul;66(1):144-52.

    Vardenafil HCl Trihydrate

    Effects of nucleotides and inhibitors on binding of 3H inhibitors to PDE5. Mol Pharmacol. 2004 Jul;66(1):144-52.


    Vardenafil HCl Trihydrate

    Effect of cGMP on [3H]vardenafil binding at 4° and 30°C. Mol Pharmacol. 2004;66(1):144-52.
     



    Vardenafil HCl Trihydrate

    Dissociation of 3H inhibitors from PDE5 after infinite dilution. Mol Pharmacol.2004 Jul;66(1):144-52.


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