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Valaciclovir HCl CMV inhibitor

Name: Valaciclovir HCl
SKU: S1876
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1876

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).

Chemical Structure

Molecular Weight: 360.8

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.83%

99.83

Related Targets	Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite Reverse Transcriptase HIV HCV Protease SARS-CoV HIV Protease Influenza Virus β-lactamase Integrase HBV Neuraminidase HCV Thioredoxin Reductase HSV RSV Enterovirus 3C-Like Protease Ribosomal Peptidyl Transferase HPV
Related Products	Bisindolylmaleimide IV Brivudine (BVDU)

Chemical Information, Storage & Stability

Molecular Weight	360.8	Formula	C₁₃H₂₀N₆O₄.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	124832-27-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)C(C(=O)OCCOCN1C=NC2=C1N=C(NC2=O)N)N.Cl

Solubility

In vitro
Batch:

Water : 72 mg/mL

DMSO : 14 mg/mL (38.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.6mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.51mg/ml (1.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15140857/ [2] https://pubmed.ncbi.nlm.nih.gov/15989601/ [3] https://pubmed.ncbi.nlm.nih.gov/8149890/ [4] https://pubmed.ncbi.nlm.nih.gov/8149891/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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