Valganciclovir HCl

Catalog No.S4050

For research use only.

Valganciclovir HCl is a prodrug for ganciclovir with antiviral activity used to treat cytomegalovirus infections.

Valganciclovir HCl Chemical Structure

CAS No. 175865-59-5

Selleck's Valganciclovir HCl has been cited by 2 Publications

Purity & Quality Control

Choose Selective CMV Inhibitors

Biological Activity

Description Valganciclovir HCl is a prodrug for ganciclovir with antiviral activity used to treat cytomegalovirus infections.
In vitro

Valganciclovir hydrochloride is a hydrochloride salt of the L-valyl ester of ganciclovir that exists as a mixture of two diastereomers. [1] After administration, these diastereomers are rapidly converted to ganciclovir by hepatic and intestinal esterases. In cytomegalovirus (CMV)-infected cells, ganciclovir is initially phosphorylated to the monophosphate form by viral protein kinase, then it is further phosphorylated via cellular kinases to produce the triphosphate form. This triphosphate form is slowly metabolized intracellularly. The phosphorylation is dependent upon the viral kinase and occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to the inhibition of viral DNA synthesis by ganciclovir triphosphate. Ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed. [2]

In vivo After oral administration, intestinal and hepatic esterases hydrolyze both diastereomers to ganciclovir, which inhibits replication of the human cytomegalovirus. Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%.[2]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 390.82
Formula

C14H22N6O5.HCl

CAS No. 175865-59-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C(C(=O)OCC(CO)OCN1C=NC2=C1N=C(NC2=O)N)N.Cl

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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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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03301415 Active not recruiting Drug: Valganciclovir Congenital Cytomegalovirus Infection National Institute of Allergy and Infectious Diseases (NIAID) April 2 2019 Phase 2
NCT03698435 Unknown status Drug: Ganciclovir|Drug: Valganciclovir Cytomegalovirus Infections University Medical Center Groningen May 25 2018 --
NCT03397706 Recruiting Drug: VRx-3996|Drug: Valganciclovir Epstein-Barr Virus Associated Lymphoma|Lymphoproliferative Disorders Viracta Therapeutics Inc. March 29 2018 Phase 1|Phase 2
NCT02606266 Terminated Drug: Valganciclovir Congenital Cytomegalovirus (CMV) Assistance Publique - Hôpitaux de Paris July 11 2017 Phase 2|Phase 3

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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