Art. -Nr.: HY-17425

Valacyclovir

(Synonyms: Valaciclovir)

1 Cited Publications

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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) .

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Reinheit: 98.50%
CAS. Nr.: 124832-26-4
Formel: C₁₃H₂₀N₆O₄
Molecular Weight:324.34

Speicherung:

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

Valacyclovir Chemical Structure

CAS. Nr.: 124832-26-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[4]

HSV-1

2.9 μg/mL (IC₅₀)

Alle HSV Isoform-spezifische Produkte anzeigen :

Alle Antibiotic Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 124832-26-4
Appearance Solid
Molecular Weight 324.34
Formel C₁₃H₂₀N₆O₄
Color White to off-white
SMILES

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

Valaciclovir
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Journal Impact Factor

Front Pharmacol

Repurposing Clinical Drugs as AdoMetDC Inhibitors Using the SCAR Strategy. [Abstract]

2020 Mar 11:11:248. PMID: 32218733

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Valacyclovir

1 Cited Publications

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Valacyclovir

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Publications Citing Use of MedChemExpress (MCE) Valacyclovir

Alle HSV Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Valacyclovir

Antibacterial Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Rare Diseases Drug Library

Pediatric Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Off-patent Drug Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

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FDA-Approved Drug Library Plus

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Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Valacyclovir

Alle HSV Isoform-spezifische Produkte anzeigen

Alle Antibiotic Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Valacyclovir Related Classifications

HY-17425 Related Classifications