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Penciclovir

Penciclovir

产品编号 T1643   CAS 39809-25-1
别名: 喷昔洛韦, BRL 39123, VSA 671

Penciclovir (BRL 39123) 是一种疱疹病毒核苷类似物 DNA 聚合酶抑制剂。它作用于HSV1 和 2,IC50分别为 0.04-1.8 μg/mL 和 0.06-4.4 μg/mL。

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Penciclovir Chemical Structure
Penciclovir, CAS 39809-25-1
规格 价格/CNY 货期 数量
100 mg ¥ 328 现货
200 mg ¥ 476 现货
500 mg ¥ 786 现货
1 mL * 10 mM (in DMSO) ¥ 228 现货
其他形式的 Penciclovir:
产品目录号及名称: Penciclovir (T1643)
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选择批次  
纯度: 99.1%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Penciclovir (BRL 39123) is a Herpesvirus Nucleoside Analog DNA Polymerase Inhibitor. In HSV infected cells, penciclovir is phosphorylated by viral thymidine kinase and subsequently converted by cellular kinases into the active metabolite, penciclovir triphosphate, which competitively inhibits viral HSV polymerase by blocking deoxyguanosine triphosphate substrate binding. As a result, herpes viral DNA synthesis and replication are selectively inhibited.
靶点活性 HSV types 1:0.04-1.8 μg/mL, HSV types 2:0.06-4.4 μg/mL
体内活性 Penciclovir具有抗多种病毒疱疹的活性,如抗HHV-6A(IC50:37.9 μM)和HHV-6B(IC50:77.8 μM)。Penciclovir具有抗Ⅰ型和Ⅱ型单纯疱疹病毒的体外活性,且对水痘带状疱疹病毒也有较好作用,却不影响未感染细胞中DNA的合成。作为鸟嘌呤类似物,Penciclovir毒性低、选择性高。Penciclovir由细胞激酶转化成三磷酸盐的活性形式,与脱氧鸟苷三磷酸竞争性抑制病毒DNA聚合酶,进而抑制病毒感染细胞的DNA合成。单纯疱疹病毒Ⅰ型的相关研究显示,Penciclovir使细胞凋亡,但造成的基因毒性较小。
细胞实验 Penciclovir is dissolved with DMSO and diluted with appropriate media[2]. Human breast cancer cell lines MCF-7 and MDA-MB-435, glioblastoma U87 mg, 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].
别名 喷昔洛韦, BRL 39123, VSA 671
分子量 253.26
分子式 C10H15N5O3
CAS No. 39809-25-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 1 mg/mL (3.94 mM)

DMSO: 32 mg/mL (126.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.9485 mL 19.7426 mL 39.4851 mL 98.7128 mL
DMSO 5 mM 0.7897 mL 3.9485 mL 7.897 mL 19.7426 mL
10 mM 0.3949 mL 1.9743 mL 3.9485 mL 9.8713 mL
20 mM 0.1974 mL 0.9871 mL 1.9743 mL 4.9356 mL
50 mM 0.079 mL 0.3949 mL 0.7897 mL 1.9743 mL
100 mM 0.0395 mL 0.1974 mL 0.3949 mL 0.9871 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Earnshaw DL, et al. Antimicrob Agents Chemother, 1992, 36(12), 2747-2757. 2. Amjad M, et al. Microbiol Immunol, 2001, 45(3), 233-240. 3. Thust R, et al. Cancer Gene Ther, 2000, 7(1), 107-117. 4. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931

文献引用

1. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931
Thunberginol C Primin Epitaraxerol Cefepime Dihydrochloride Monohydrate Vasicinolone Methyl 4-Hydroxyphenylacetate Corydine 1,4,7-Eudesmanetriol

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 抗感染化合物库 ReFRAME 相关化合物库 毒性化合物库 FDA上市及药典收录分子库 抗病毒库 NO PAINS 化合物库 上市药物库 抑制剂库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Penciclovir 39809-25-1 Microbiology/Virology Proteases/Proteasome Antifection HCV Protease HSV VSA671 喷昔洛韦 BRL-39123 BRL 39123 mortality inhibit no-toxic Inhibitor VSA 671 anti-herpesvirus VSA-671 BRL39123 Herpes simplex virus inhibitor

 

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