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Acyclovir (Synonyms: ACV, BW 248U, NSC 645011)

Catalog No.GC17186

Acyclovir is a potent oral antiviral drug. Acyclovir has anti-herpetic activity with IC50 values ​​of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir induces cell cycle disruption and apoptosis.

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Acyclovir Chemical Structure

Cas No.: 59277-89-3

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10mM (in 1mL DMSO)
$27.00
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25mg
$24.00
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50mg
$39.00
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100mg
$62.00
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500mg
$105.00
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Sample solution is provided at 25 µL, 10mM.

Description of Acyclovir

Acyclovir is a potent oral antiviral drug. Acyclovir has anti-herpetic activity with IC50 values ​​of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir induces cell cycle disruption and apoptosis[1] [2].

In the plaque reduction assay (PRA) of Vero cells, Acyclovir (20μM; 3d) treatment showed 100% plaque inhibition[1]. Acyclovir (10-100μM; 24-72h) blocks DNA synthesis, thereby arresting the cell cycle at G2/M and S phases and increasing the G1 hypodiploid peak in a dose-dependent manner. Acyclovir (10-100μM; 24-72h) induces apoptosis through activation of caspase-3 and the presence of nuclear DNA fragmentation[2].

Treatment of infected mice with Acyclovir (20mg/kg; po; three times daily; 10d) inhibited the development of skin lesions and led to a dissociation between the DTH response and antibody production [3]. In the Acyclovir-induced nephrotoxicity model, after mice were given Acyclovir (150, 600 mg/kg; ip; 9d), serum creatinine and urea nitrogen levels increased, histopathological changes occurred in the kidneys of mice, and the expression levels of vascular endothelial growth factor (VEGF) and its receptor VEGFR2 were reduced[4].

References:
[1]. Musarra-Pizzo M, Pennisi R, Ben-Amor I, et al. In vitro anti-HSV-1 activity of polyphenol-rich extracts and pure polyphenol compounds derived from pistachios kernels (Pistacia vera L.)[J]. Plants, 2020, 9(2): 267.
[2].Suzuki M, Okuda T, Shiraki K. Synergistic antiviral activity of Acyclovir and vidarabine against herpes simplex virus types 1 and 2 and varicella-zoster virus[J]. Antiviral research, 2006, 72(2): 157-161.
[3]. Benedetti S, Catalani S, Palma F, et al. Acyclovir induces cell cycle perturbation and apoptosis in Jurkat leukemia cells, and enhances chemotherapeutic drug cytotoxicity[J]. Life sciences, 2018, 215: 80-85.
[4].Lu H, Han Y J, Xu J D, et al. Proteomic characterization of acyclovir-induced nephrotoxicity in a mouse model[J]. PLoS One, 2014, 9(7): e103185.

Protocol of Acyclovir

Cell experiment [1]:

Cell lines

Vero cells

Preparation Method

Vero cells were infected with HSV-1 for 1h and then treated with NPRE (0.1, 0.2, 0.4, 0.6, 0.8mg/mL). The DMSO was used in the control samples and Acyclovir (20µM) was used as positive control.

Reaction Conditions

20μM; 3d.

Applications

Treatment with 20μM Acyclovir showed 100% plaque inhibition.
Animal experiment [2]:
ModelNephrotoxicity Model

Preparation Method

ICR mice were randomly divided into three groups to receive saline, 150mg/kg Acyclovir, or 600mg/kg Acyclovir once-daily for 9 days. Mice were kept at room temperature and 70±10% humidity, with a light-dark cycle. Food and water were available ad libitum. Acyclovir was administered intraperitoneally (ip) diluted in 20mL/kg of 0.9% sodium chloride injection solution. The saline group received an equal volume of the 0.9% sodium chloride solution.

Dosage form

150,600mg/kg; ip; 9d

Applications

After administration of Acyclovir, levels of serum creatinine and urea nitrogen increased ,mouse kidneys exhibited histopathological changes and reduced expression levels of vascular endothelial growth factor (VEGF) and its receptor VEGFR2.

References:
[1]. Musarra-Pizzo M, Pennisi R, Ben-Amor I, et al. In vitro anti-HSV-1 activity of polyphenol-rich extracts and pure polyphenol compounds derived from pistachios kernels (Pistacia vera L.)[J]. Plants, 2020, 9(2): 267.
[2]. Lu H, Han Y J, Xu J D, et al. Proteomic characterization of acyclovir-induced nephrotoxicity in a mouse model[J]. PLoS One, 2014, 9(7): e103185.

Chemical Properties of Acyclovir

Cas No. 59277-89-3 SDF
Synonyms ACV, BW 248U, NSC 645011
Chemical Name 2-amino-9-(2-hydroxyethoxymethyl)-3H-purin-6-one
Canonical SMILES C1=NC2=C(N1COCCO)NC(=NC2=O)N
Formula C8H11N5O3 M.Wt 225.21
Solubility ≥ 11.4mg/mL in DMSO Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Acyclovir

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 4.4403 mL 22.2015 mL 44.403 mL
5 mM 0.8881 mL 4.4403 mL 8.8806 mL
10 mM 0.444 mL 2.2202 mL 4.4403 mL
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In vivo Formulation Calculator (Clear solution) of Acyclovir

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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.
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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