Vardenafil HCl Trihydrate
Catalog #
27776-1
$460
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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.
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Synonyms
2-[2-Ethoxy-5-(4-ethyl-piperazine-1-sulfonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one monohydrochloride trihydrate
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Product Data Gallery
Product Info
Storage and Usage
Citations
Format
nearly colourless solid
Target(s)
PDE5
Formula
C23H32N6O4S • HCl • 3 >H2O
MW
579.1 Da
Solubility
Soluble in ethanol or 0.1M HCl. Only slightly soluble in water.
Biological Activity
Vardenafil has shown a greater selective inhibition towards PDE5 (IC50 = 0.7 nM) vs. PDEs from bovine, with the IC50 values of 180 nM, >10 µM, 2.5 µM, 4 µM and 11 nM for PDE1, PDE2, PDE3, PDE4 and PDE6, respectively. It is shows selectivity for PDE5 vs. over 300-fold relative to PDE11 and over 1000-fold relative to PDEs 8, 9, and 10.
CAS Registry #
224785-90-4
Background
Vardenafil is frequently used in the treatment erectile dysfunction, and is the active ingredient in Levitra. It 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.
References
Saenz de Tejada I., et al. Int J Impot Res. 2001 Oct;13(5):282-90.
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