GLPBio

Vardenafil HCl Trihydrate

Catalog No.: GC10588Purity:>98%
COASDSData Sheet
An inhibitor of PDE5 and PDE6

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Vardenafil HCl Trihydrate
Cas No.: 330808-88-3
10mM (in 1mL DMSO)In Stock
$57.00
1
10mgIn Stock
$43.00
1
100mgIn Stock
$294.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

Citas (Citations)

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    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
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    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

Descripción (Description)

Vardenafil is a potent and selective inhibitor of phosphodiesterase type5 (PDE5) with the IC50 value of 0.7 nM in enzymatic assay in vitro [1]. Vardenafil HCl Trihydrate is a salt form of vardenafil. [1]

Vardenafil has shown a greater selective inhibition towards PDE5 than PDEs from bovine, with the IC50 values of 180nM,>10000nM, 2500nM, 4000nM and 11nM for PDE1, PDE2, PDE3, PDE4 and PDE6, respectively. Besides, Vardenafil has been reported to significantly enhance the SNP-induced, ACh-induced and transmural electrical stimulation-induced relaxation of human trabecular smooth muscle. Vardenafil has been revealed to increase the amount of cGMP in human corpus cavernosum. Apart from these, Vardenafil has also enhanced the length of penile in the conscious rabbit [1].

Reference:
[1] Saenz de Tejada I1, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, Körschen HG, Niewöhner U, Haning H, Pages E, Bischoff E.The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90.

Protocolo (Protocol)

Kinase experiment [1]:

Enzyme inhibition assays

PDE5 and 3H-cGMP were added in DMSO (final concentration of DMSO 0.1%). Incubation period was 15 min at 30 ℃. All tests were done in duplicate and were repeated at least three times. The IC50 value for the PDE5 inhibition were determined from sigmoidal curves, fitted to plots of enzyme activity vs log compound concentration using a GraphPad curve fitting program.
Cell experiment [1]:

Cell lines

Human trabecular smooth muscle cells

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

3, 10 or 30 nM

Applications

In human trabecular smooth muscle strips, Vardenafil HCl Trihydrate significantly enhanced SNP-induced relaxation.
Animal experiment [1]:

Animal models

A conscious rabbit model

Dosage form

0.1, 0.3, 1 or 3 mg/kg; p.o.

Applications

In a conscious rabbit model, Vardenafil HCl Trihydrate dose-dependently potentiated erectile responses induced by SNP.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Saenz de Tejada I1, Angulo J, Cuevas P, Fernández A, Moncada I, Allona A, Lledó E, K?rschen HG, Niew?hner U, Haning H, Pages E, Bischoff E.The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001 Oct;13(5):282-90.

Propiedades químicas (Chemical Properties)

N.º CAS
330808-88-3
Nombre químico
2-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one
SMILES
CCCC1=NC(=C2N1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C
Fórmula molecular
C23H32N6O4S.HCl.3H2O
Peso molecular
579.11
Solubilidad
≥ 13.3 mg/mL in DMSO, ≥ 3.42 mg/mL in EtOH with ultrasonic and warming, ≥ 95 mg/mL in Water
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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