Home Microbiology CMV inhibitor Valaciclovir HCl For research use only.

Valaciclovir HCl

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).

Valaciclovir HCl Chemical Structure

Valaciclovir HCl Chemical Structure

CAS No. 124832-27-5

Purity & Quality Control

Valaciclovir HCl Related Products

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
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00169416 Completed
Varicella
GlaxoSmithKline
 March 2005 Phase 3

Chemical Information & Solubility

Molecular Weight 360.8 Formula

C13H20N6O4.HCl
CAS No. 124832-27-5 SDF Download Valaciclovir HCl SDF
Smiles CC(C)C(C(=O)OCCOCN1C=NC2=C1N=C(NC2=O)N)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 72 mg/mL

DMSO : 14 mg/mL ( (38.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

Handling Instructions

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