An inhibitor of PDE5 and PDE6
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Vardenafil (hydrochloride hydrate)

Item No. 14930

Technical Information
Formal Name
2-[2-ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-5-methyl-7-propyl-imidazo[5,1-f][1,2,4]triazin-4(1H)-one, monohydrochloride trihydrate
CAS Number
330808-88-3
Molecular Formula
C23H32N6O4S • HCl [3H2O]
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 0.3 mg/mlDMSO: 2 mg/mlEthanol: 0.5 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
215 nm
SMILES
CC(N=C1CCC)=C2N1N([H])C(C3=CC(S(=O)(N4CCN(CC)CC4)=O)=CC=C3OCC)=NC2=O.Cl.O.O.O
InChi Code
InChI=1S/C23H32N6O4S.ClH.3H2O/c1-5-8-20-24-16(4)21-23(30)25-22(26-29(20)21)18-15-17(9-10-19(18)33-7-3)34(31,32)28-13-11-27(6-2)12-14-28;;;;/h9-10,15H,5-8,11-14H2,1-4H3,(H,25,26,30);1H;3*1H2
InChi Key
FBCDRHDULQYRTB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Vardenafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC50s = 0.2-1.2 nM) and PDE6 (IC50 = 2 nM).1,2,3 It is selective for PDE5 and PDE6 over PDE1 and PDE11 (IC50s = 230 and 130 nM, respectively). Vardenafil (4 mg/kg per day for three weeks) improves erectile function in a rat model of acute arteriogenic erectile dysfunction by increasing intracavernous pressure and mean arterial pressure, and this effect persists for at least two weeks following the end of treatment.4 Chronic vardenafil administration at a dose of 2 mg/kg for five weeks in subordinate mice reduces the latency to mount and increases the frequency of mounting behavior.5 Formulations containing vardenafil have been used in the treatment of erectile dysfunction.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Card, G.L., England, B.P., Suzuki, Y., et alStructural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12(12), 2233-2247 (2004).

    2. Boyle, C.D., Xu, R., Asberom, T., et alOptimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED. Bioorg. Med. Chem. Lett. 15(9), 2365-2369 (2005).

    3. Smith, W.B., II, McCaslin, I.R., Gokce, A., et alPDE5 inhibitors: Considerations for preference and long-term adherence. Int. J. Clin. Pract. 67(8), 768-780 (2013).

    4. Hotta, Y., Ohno, R., Kataoka, T., et alEffects of chronic vardenafil treatment persist after end of treatment in rats with acute arteriogenic erectile dysfunction. J. Sex Med. 9(7), 1782-1788 (2012).

    5. Dadomo, H., Parmigiani, S., Nicolini, Y., et alRepeated and chronic administration of Vardenafil or Sildenafil differentially affects emotional and socio-sexual behavior in mice. Behav. Brain Res. 253, 103-112 (2013).