Vardenafil-d5 (hydrochloride)

Vardenafil-d5 (hydrochloride)

• UNSPSC Description: Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4[1]. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
• Target Antigen: Endogenous Metabolite; Isotope-Labeled Compounds; Phosphodiesterase (PDE)
• Type: Isotope-Labeled Compounds
• Related Pathways: Metabolic Enzyme/Protease;Others
• Applications: Metabolism-protein/nucleotide metabolism
• Field of Research: Endocrinology; Metabolic Disease; Inflammation/Immunology
• Solubility: 10 mM in DMSO
• Smiles: CC1=C2N(NC(C3=CC(S(=O)(N4CCN(CC4)C([2H])(C([2H])([2H])[2H])[2H])=O)=CC=C3OCC)=NC2=O)C(CCC)=N1.Cl
• Molecular Weight: 530.09
• References & Citations: [1]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. |[2]Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.|[3]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.|[4]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.|[5]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. |[6]Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31(3). |[7]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported