Valaciclovir HCl

For research use only.

Catalog No.S1876

Valaciclovir HCl Chemical Structure

CAS No. 124832-27-5

Valaciclovir HCl, an aciclovir prodrug, inhibits activity of virus DNA polymerase, used to treat infections caused by herpes simplex virus (HSV) and varicella zoster virus, and for prophylaxis against cytomegalovirus (CMV).

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 127 In stock
EUR 95 In stock
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Biological Activity

Description Valaciclovir HCl, an aciclovir prodrug, inhibits activity of virus DNA polymerase, used to treat infections caused by herpes simplex virus (HSV) and varicella zoster virus, and for prophylaxis against cytomegalovirus (CMV).
Targets
DNA polymerase [1]
In vitro

Valaciclovir inhibits the uptake of substrates of dipeptide transporters, such as cefalexin. The metabolism of Valaciclovir to Aciclovir probably occurs within the gut lumen prior to absorption, in the small intestine after uptake but before entry into the portal blood system, and in the liver before entry into systemic circulation. [1] Valaciclovir (Valtrex, Zelitrex), the L-valine ester of aciclovir, increases aciclovir bioavailability by 3- to 5-fold over that achievable with oral aciclovir. Valaciclovir extends the efficacy of aciclovir in the treatment of herpes zoster and genital HSV infections, using less frequent dose regimens but retaining the highly acceptable safety profile established for aciclovir. Valaciclovir is rapidly absorbed and extensively converted to aciclovir and L-valine, the essential amino acid after oral administration. [2]

In vivo Valaciclovir, the L-valyl ester of acyclovir (ZOVIRAX), demonstrates good oral absorption and nearly complete conversion to acyclovir incynomolgus monkeys, indicating its suitability as an orally administered prodrug. [3] Valaciclovir demonstrates good oral absorption, rapid distribution and elimination, and extensive biotransformation to acyclovir in male CD rats. Valaciclovir is more efficiently metabolized when administered orally, indicating first-pass intestinal and/or hepatic metabolism. Rapid hydrolysis of Valaciclovir in rat liver and intestinal homogenates further suggested the significance of presystemic metabolism. [4]

Protocol

Solubility (25°C)

In vitro Water 72 mg/mL (199.55 mM)
DMSO 14 mg/mL (38.8 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 360.8
Formula

C13H20N6O4.HCl

CAS No. 124832-27-5
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)C(C(=O)OCCOCN1C=NC2=C1N=C(NC2=O)N)N.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02997982 Completed Drug: Valaciclovir 500Mg Tablet Alzheimer Disease|Mild Cognitive Impairment|Herpes Simplex Hugo Lovheim|Umeå University December 2016 Phase 2
NCT01633476 Unknown status Drug: Valaciclovir ANCA Associated Vasculitis|CMV Infection Professor Lorraine Harper|Wellcome Trust|University of Birmingham July 2013 Phase 2
NCT01364792 Completed Drug: Valaciclovir Schizophrenia|Psychosis University Medical Center Groningen|Stanley Medical Research Institute April 2011 Phase 2
NCT01390805 Completed Drug: Valaciclovir Hydrochloride. Genital Herpes GlaxoSmithKline November 2006 --
NCT00169416 Completed Drug: valaciclovir HCl granules Varicella GlaxoSmithKline March 2005 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID