| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Penciclovir (BRL-39123) is a guanosine analogue used as an antiviral drug for the treatment of various herpesvirus infections. It has activity against HSV types 1 and 2 with IC50 of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively. As a nucleoside analogue, Penciclovir exhibits low toxicity and good selectivity. Penciclovir is absorbed poorly when given orally, thus it is used as a topical treatment, and is the active ingredient in the cold sore medications such as Denavir, Vectavir and Fenivir.
| Targets |
HSV-1(EC50=0.5 μg/mL);HSV-2(EC50=0.8 μg/mL)
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|---|---|
| ln Vitro |
With EC50s of 0.5, 0.8, 2.4, 52, 100, 1.2, 1.6, 0.9, >100 µg/ml for HSV-1 (HFEM), HSV-2 (MS), VZV (Ellen), CMV (AD-169), BHV-1 (Oxford 1964), BHV-2 (New York 1), EHV-1 (Quai Hals), FHV-1 (B927), and SVV, respectively, penciclovir (0-100 µg/ml) exhibits anti-herpesvirus activity.To human cells that are not infected, penciclovir (0-100 µg/ml) exhibits no toxicity[1].
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| ln Vivo |
Penciclovir (100 mg/kg; s.c.; daily for 5 days) preventes mortality in mouse[2].
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| Cell Assay |
Human breast cancer cell lines MCF-7 and MDA-MB-435, glioblastoma U87MG, and embryonic kidney cells 293T are cultured at 37°C in a humidified atmosphere containing 5% CO2 in Iscove’s modified Dulbecco medium or Leibovitz’s L-medium and 5% fetal bovine serum (FBS). The assays are performed with slight modifications. In brief, cells are seeded into 24-well plates (5×104 cells/well) and infected 48 h later with 103 particles per cell of unmodified virus (Adtk), PEGylated virus (PEG-Adtk), or RGD-PEG-modified virus (RGD-PEG-Adtk) in triplicates in culture medium with 2% FBS and incubated for 4 h at 37°C. The incubation medium is then replaced by normal medium and cells are further incubated for 48 h. Cells are harvested and lysed with 500 μL of TK lysis buffer that contained 0.5% Nonidet P-40 (NP-40), 20 mM N-(2-hydroxyethyl) piperazine-N′-(2-ethanesulfonic acid) (HEPES) (pH 7.6), 2 mM Mg(OAc)2, 1 mM dithiothreitol, and 50 μM thymidine. The supernatant is collected after centrifugation. The samples are kept at -80°C until use. The modified and unmodified adenovirus protein concentrations are determined by the Micro BCA assay. One microgram of cell extract is incubated with HSV1-tk substrate 8-3H-Penciclovir (8-3 H-PCV). The phosphorylated tracer is separated from unphosphorylated 8-3 H-PCV with DE-81 filters. TK activity is expressed as the percentage of conversion of substrate per minute per microgram protein.
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| Animal Protocol |
Animal Model: Three-week-old female Balb/c mice[2]
Dosage: 100 mg/kg Administration: S.c.; daily for 5 days Result: decreased viral titres in the respiratory systems of mice infected with PR3 and W/t. |
| References |
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| Molecular Formula |
C10H15N5O3
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|---|---|
| Molecular Weight |
253.26
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| Exact Mass |
253.11749
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| Elemental Analysis |
C, 47.42; H, 5.97; N, 27.65; O, 18.95
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| CAS # |
39809-25-1
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| Related CAS # |
Penciclovir-d4;1020719-72-5;Penciclovir sodium;97845-62-0
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| Appearance |
Solid powder
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| SMILES |
C1=NC2=C(N1CCC(CO)CO)N=C(NC2=O)N
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| InChi Key |
JNTOCHDNEULJHD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H15N5O3/c11-10-13-8-7(9(18)14-10)12-5-15(8)2-1-6(3-16)4-17/h5-6,16-17H,1-4H2,(H3,11,13,14,18)
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| Chemical Name |
2-amino-9-[4-hydroxy-3-(hydroxymethyl)butyl]-3H-purin-6-one
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| Synonyms |
BRL-39123; BRL 39123; BRL39123; VSA 671; VSA671; VSA-671; Penciclovir; Denavir, Vectavir and Fenivir.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 25~34 mg/mL (98.71~134.24 mM)
H2O : ~2 mg/mL (~7.90 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (9.87 mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9485 mL | 19.7426 mL | 39.4851 mL | |
| 5 mM | 0.7897 mL | 3.9485 mL | 7.8970 mL | |
| 10 mM | 0.3949 mL | 1.9743 mL | 3.9485 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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