Penciclovir-BRL-39123-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPenciclovirCat. No.: HY-17424CAS No.: 39809-25-1Synonyms: BRL 39123; VSA 671分式: CHNO分量: 253.26作靶点: HSV作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 53 mg/mL (209.27 mM)

2、* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9485 mL 19.7426 mL 39.4851 mL5 mM 0.7897 mL 3.9485 mL 7.8970 mL10 mM 0.3949 mL 1.9743 mL 3.9485 mL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，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Penciclovir 有效作于 HSV1 和 2，IC50 分别为 0.04-1.

3、8 g/mL 和 0.06-4.4 g/mL。IC50 & Target IC50: 0.04-1.8 g/mL (HSV-1), 0.06-4.4 g/mL (HSV-2), 1.6-8 g/mL (VZV), 1.5-3.1 g/mL (EBV), 51 g/mL(HCMV) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Penciclovir inhibits herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2), varicella-zoster virus (VZV

4、),epstein-Barr virus (EBV), human cytomegalovirus (HCMV) with IC50 of 0.04-1.8 g/mL, 0.06-4.4 g/mL,1.6-8g/mL, 1.5-3.1 g/mL, 51 g/mL, respectively. Penciclovir (PCV) is an acyclic guanine derivative (which isnot commercially available as an oral agent), has a spectrum of activity and a mechanism of a

5、ction similar tothose of acyclovir (ACV) 1.PROTOCOLCell Assay 2 Human breast cancer cell lines MCF-7 and MDA-MB-435, glioblastoma U87MG, and embryonic kidney cells293T are cultured at 37C in a humidified atmosphere containing 5% CO2 in Iscoves modified Dulbeccomedium or Leibovitzs L-medium and 5% fe

6、tal bovine serum (FBS). The assays are performed with slightmodifications. In brief, cells are seeded into 24-well plates (5104 cells/well) and infected 48 h later with 103particles per cell of unmodified virus (Adtk), PEGylated virus (PEG-Adtk), or RGD-PEG-modified virus (RGD-PEG-Adtk) in triplicat

7、es in culture medium with 2% FBS and incubated for 4 h at 37C. The incubationmedium is then replaced by normal medium and cells are further incubated for 48 h. Cells are harvested andlysed with 500 L of TK lysis buffer that contained 0.5% Nonidet P-40 (NP-40), 20 mM N-(2-hydroxyethyl)piperazine-N-(2

8、-ethanesulfonic acid) (HEPES) (pH 7.6), 2 mM Mg(OAc)2, 1 mM dithiothreitol, and 50 Mthymidine. The supernatant is collected after centrifugation. The samples are kept at -80C until use. Themodified and unmodified adenovirus protein concentrations are determined by the Micro BCA assay. Onemicrogram o

9、f cell extract is incubated with HSV1-tk substrate 8-3H-Penciclovir (8-3 H-PCV). Thephosphorylated tracer is separated from unphosphorylated 8-3 H-PCV with DE-81 filters. TK activity isexpressed as the percentage of conversion of substrate per minute per microgram protein 2.MCE has not independently

10、 confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Piret J, et al. Resistance of herpes simplex viruses to nucleoside analogues: mechanisms, prevalence, and management. AntimicrobAgents Chemother. 2011 Feb;55(2):459-72.2. Xiong Z, et al. Imaging chemically modified adenovirus for targeting tumors expressing integrin alphavbeta3 in living micewith mutantherpes simplex virus type 1 thymidine kinase PET reporter gene. J Nucl Med. 2006 Jan;47(1):130-9.McePdfHeightCaution: Product has not been f