| Bioactivity | 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]. |
| Invitro | 氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱[1]。Vardenafil hydrochloride 特异性抑制 PDE5 对 cGMP 的水解，IC50 为 0.7 nM[2]。Vardenafil hydrochloride 增加阴茎海绵体组织中的细胞内 cGMP 水平，从而导致身体鼻窦扩张和血流量增加[4]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Vardenafil-d5 hydrochloride 相关抗体: |
| In Vivo | Vardenafil hydrochloride (IV；0.03 mg/kg) 对海绵体神经损伤大鼠具有促进作用[5]。Vardenafil hydrochloride (IV；0.17 mg/kg，每天一次；7 天) 保护肝脏对抗 Con A 诱导的肝炎，并降低肝组织中 NF-[6]。Vardenafil hydrochloride (口服；10 mg/kg，每日一次；25 周) 防止组织 cGMP 水平的降低和 ZDF 心脏中 3-NT 生成的增加[7]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| Formula | C23H28D5ClN6O4S |
| Molar Mass | 530.09 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [2]. 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. [3]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544. [4]. 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. [5]. 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. [6]. 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. [7]. Ahmed N, et al. Hepatoprotective role of vardenafil against experimentally induced hepatitis in mice. J Biochem Mol Toxicol. 2017 Mar. 31(3). |
Vardenafil-d5 hydrochloride
CAS: F: C23H28D5ClN6O4S W: 530.09
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a se
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This product is for research use only, not for human use. We do not sell to patients.