Penciclovir
(Synonyms: 喷昔洛韦; BRL 39123; VSA 671) 目录号 : GC17848An antiviral guanosine analog
Cas No.:39809-25-1
Sample solution is provided at 25 µL, 10mM.
Penciclovir is an inhibitor of HSV-1 DNA synthesis [1].
Penciclovir is a guanine derivative and is used as a drug for the treatment against herpesviruses. Penciclovir has a similar spectrum of activity with acyclovir. In the plaque reduction assay, penciclovir shows potent inhibitory activities against HSV-1, HSV-2 and VZV with IC50 values of 0.4μg/ml, 1.5μg/ml and 3.1μg/ml, respectively. It also shows minimal activity against CMV. In MRC-5 cells, penciclovir inhibits the replication of HSV-1 with IC99 value of 0.4μg/ml. Moreover, penciclovir exerts persistent antiviral activity against HSV-1and HSV-2 in Vero cells. Besides that, penciclovir is found to be phosphorylated to the triphosphate in HSV-1-infected MRC-5 cells. The penciclovir triphosphate is the metabolite that actually inhibits herpesvirus replication. Penciclovir inhibits HSV-1 DNA synthesis with IC50 value of 0.16μM without effect on cellular DNA synthesis [1, 2].
References:
[1] Boyd M R, Bacon T H, Sutton D, et al. Antiherpesvirus activity of 9-(4-hydroxy-3-hydroxy-methylbut-1-yl) guanine (BRL 39123) in cell culture. Antimicrobial agents and chemotherapy, 1987, 31(8): 1238-1242.
[2] Hodge R A, Perkins R M. Mode of action of 9-(4-hydroxy-3-hydroxymethylbut-1-yl) guanine (BRL 39123) against herpes simplex virus in MRC-5 cells. Antimicrobial agents and chemotherapy, 1989, 33(2): 223-229.
Cell experiment: |
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[2]. |
References: [1]. Piret J, et al. Resistance of herpes simplex viruses to nucleoside analogues: mechanisms, prevalence, and management. Antimicrob Agents Chemother. 2011 Feb;55(2):459-72. |
Cas No. | 39809-25-1 | SDF | |
别名 | 喷昔洛韦; BRL 39123; VSA 671 | ||
化学名 | 2-amino-9-[4-hydroxy-3-(hydroxymethyl)butyl]-3H-purin-6-one | ||
Canonical SMILES | C1=NC2=C(N1CCC(CO)CO)NC(=NC2=O)N | ||
分子式 | C10H15N5O3 | 分子量 | 253.26 |
溶解度 | ≥ 11.95mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 | 7.897 mL |
10 mM | 0.3949 mL | 1.9743 mL | 3.9485 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet