Valacyclovir (Synonyms: Valaciclovir)

Name: Valacyclovir
Brand: MedChemExpress
SKU: HY-17425
Rating: 4.5 (1 reviews)

Cat. No.: HY-17425 Purity: 98.50%: Data Sheet
COA

SDS
Handling Instructions
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Valacyclovir (Valaciclovir) is an orally active antiviral agent for herpes simplex, herpes zoster, and herpes B. Valacyclovir inhibits HSV-1 W (₅₀=2.9 μg/ml). Valacyclovir is a proagent of Aciclovir (HY-17422) .

For research use only. We do not sell to patients.

Valacyclovir Chemical Structure

CAS No. : 124832-26-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Valacyclovir:

Valacyclovir hydrochloride In-stock
Valacyclovir hydrochloride hydrate Get quote

1 Publications Citing Use of MCE Valacyclovir

•Front Pharmacol. 2020 Mar 11;11:248. [Abstract]

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[4]

HSV-1

2.9 μg/mL (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1100 μM Compound: Valacyclovir	TP_TRANSPORTER: inhibition of Gly-Sar uptake, L-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells TP_TRANSPORTER: inhibition of Gly-Sar uptake, L-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	[PMID: 9706043]
CHO	IC₅₀	3400 μM Compound: Valacyclovir	TP_TRANSPORTER: inhibition of Gly-Sar uptake, D-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells TP_TRANSPORTER: inhibition of Gly-Sar uptake, D-form (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	[PMID: 9706043]
CHO	IC₅₀	400 μM Compound: L-Valyl ester of Zidovudine	TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells	[PMID: 9706043]
HeLa	IC₅₀	1.42 mM Compound: valacyclovir	Inhibition of human PEPT1-mediated [3H]Gly-Sar uptake in human HeLa cells Inhibition of human PEPT1-mediated [3H]Gly-Sar uptake in human HeLa cells	[PMID: 19957998]
HeLa	IC₅₀	431 μM Compound: Valacyclovir	Inhibitory concentration against [3H]glycylsarcosine uptake in HeLa cells expressing human Intestinal peptide transporter PepT1 Inhibitory concentration against [3H]glycylsarcosine uptake in HeLa cells expressing human Intestinal peptide transporter PepT1	[PMID: 15715497]

In Vitro

Valacyclovir (Valaciclovir; VACV) uptake was concentration dependent and saturable with a Michaelis-Menten constant and maximum velocity of 1.64 mM and 23.34 nmol/mg protein/5 min, respectively. A very similar Km value was obtained in hPEPT1/CHO cells and in rat and rabbit tissues and Caco-2 cells, suggesting that hPEPT1 dominates the intestinal transport properties of VACV in vitro^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

For treatment of a first episode of genital herpes, a large comparative trial has shown that Valacyclovir (1 g twice a day) is as effective as acyclovir (200 mg five times a day) when given for 10 days. For treating recurrences, two trials show that valacyclovir is as effective as acyclovir (200 mg five times a day) with a treatment period of 5 days. A daily dose of 1 g of valacyclovir is as effective as 2 g daily. Valacyclovir can be administered once a day^[1].
The concentrations of acyclovir in serum and CSF were measured at steady state after 6 days of oral treatment with 1,000 mg of valacyclovir three times a day^[2].
EC50 values of PE and AC in 3T3 cells were 0.02 and 0.01 ug/ml, while values in BHK cells were 0.2 and 0.03 ug/ml. Treatment of infected immunosuppressed mice and FA and VA (b.i.d., 5.5 days) reduced the proportion with erythema from 100% to 24% and 38%, and eliminated ear paralysis, ear lesions (vesicles, etc) and death. Virus was absent from ear and brainstem by day 6, but reappeared after discontinuation in mice treated with VA^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

324.34

Formula

C₁₃H₂₀N₆O₄

CAS No.

124832-26-4

Appearance

Solid

Color

White to off-white

SMILES

N[C@@H](C(C)C)C(OCCOCN1C=NC2=C1N=C(N)NC2=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (308.32 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0832 mL	15.4159 mL	30.8318 mL
5 mM	0.6166 mL	3.0832 mL	6.1664 mL
10 mM	0.3083 mL	1.5416 mL	3.0832 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.50%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) HNMR (135 KB) RP-HPLC (169 KB) LCMS (106 KB)

Handling Instructions (2659 KB)

References

[1]. Valacyclovir. New indication: for genital herpes, simpler administration. Can Fam Physician. 1999 Jul;45:1698-700, 1703-5. [Content Brief]

[2]. Lycke J, et al. Acyclovir levels in serum and cerebrospinal fluid after oral administration of valacyclovir. Antimicrob Agents Chemother. 2003 Aug;47(8):2438-41. [Content Brief]

[3]. Comparison of efficacies of famciclovir and valaciclovir against herpes simplex virus type 1 in a murineimmunosuppression model. Antimicrob Agents Chemother. 1995 May;39(5):1114-9. [Content Brief]

[4]. Dhaliwal DK, Romanowski EG, Yates KA, Valacyclovir inhibits recovery of ocular HSV-1 after experimental reactivation by excimer laser keratectomy. Cornea. 1999 Nov;18(6):693-9. [Content Brief]

[5]. Guo A, Hu P, Balimane PV, Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.J Pharmacol Exp Ther. 1999 Apr;289(1):448-54. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0832 mL	15.4159 mL	30.8318 mL	77.0796 mL
	5 mM	0.6166 mL	3.0832 mL	6.1664 mL	15.4159 mL
	10 mM	0.3083 mL	1.5416 mL	3.0832 mL	7.7080 mL
	15 mM	0.2055 mL	1.0277 mL	2.0555 mL	5.1386 mL
	20 mM	0.1542 mL	0.7708 mL	1.5416 mL	3.8540 mL
	25 mM	0.1233 mL	0.6166 mL	1.2333 mL	3.0832 mL
	30 mM	0.1028 mL	0.5139 mL	1.0277 mL	2.5693 mL
	40 mM	0.0771 mL	0.3854 mL	0.7708 mL	1.9270 mL
	50 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5416 mL
	60 mM	0.0514 mL	0.2569 mL	0.5139 mL	1.2847 mL
	80 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9635 mL
	100 mM	0.0308 mL	0.1542 mL	0.3083 mL	0.7708 mL

Valacyclovir Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Valacyclovir124832-26-4ValaciclovirHSVAntibioticBacterialHerpes simplex virusInhibitorinhibitorinhibit

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Valacyclovir (Synonyms: Valaciclovir)

Customer Review

Other Forms of Valacyclovir:

Valacyclovir Related Antibodies

1 Publications Citing Use of MCE Valacyclovir

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HSV Isoform Specific Products:

View All Antibiotic Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Valacyclovir Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Valacyclovir Related Classifications

Keywords:

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Customer Review

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