Ganciclovir-BW-759-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGanciclovirCat. No.: HY-13637CAS No.: 82410-32-0Synonyms: BW 759; 2-Nor-2-deoxyguanosine分式: CHNO分量: 255.23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 : 60 mg/mL

2、 (235.08 mM; Need ultrasonic)H2O : 3.67 mg/mL (14.38 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.9180 mL 19.5902 mL 39.1803 mL5 mM 0.7836 mL 3.9180 mL 7.8361 mL10 mM 0.3918 mL 1.9590 mL 3.9180 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。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配

3、制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (11.75 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (11.75 mM); Clear solution1/3 Mast

4、er of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3 mg/mL (11.75 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ganciclovir是有效的单纯疱疹病毒 (HSV) 抑制剂，包括巨细胞病毒（CMV），抑制FHV-1的 IC50 值为5.2 M。IC50 & Target IC50: 5.2 M (FHV-1) 1体外研究 Ganciclovir is an acyclic deoxyguanosine analog

5、structurally similar to acyclovir but with superior activityagainst CMV. The median ganciclovir concentration required to inhibit viral replication by 50 percent is 2.15mumol versus 72 mumol for acyclovir 2.The primary mechanism of ganciclovir action against CMV isinhibition of the replication of vi

6、ral DNA by ganciclovir-5-triphosphate (ganciclovir-TP). This inhibition includesa selective and potent inhibition of the viral DNA polymerase.Ganciclovir is metabolized to the triphosphateform by primarily three cellular enzymes: a deoxyguanosine kinase induced by CMV-infected cells; guanylatekinase

7、; and phosphoglycerate kinase 3.体内研究 In adult rats, the intracochlear diffusion of ganciclovir is shown to achieve the same concentration as inblood. In gestating mice, transplacental diffusion is observed, with a fetal-to-maternal blood ratio of 0.5. Innewborn mice, the plasma concentration profile

8、 of ganciclovir shows a peak at 2 h followed by a gradualdecrease. In adult mice, the concentration peaked at 1 h, but becomes undetectable by 2 h after injection.Counts of white blood cells, red blood cells and platelets decreases significantly in ganciclovir-treatednewborn mice 4.PROTOCOLAnimal Ra

9、ts: Two albino rats non-immunized for MCMV are used in the study. After being weighed, two adult ratsAdministration 4 undergo peritoneal injections. The first rat receives 50 mg/kg of ganciclovir twice a day (i.e. 100 mg/kg/day),for a total of 3 days or 6 injections. The second rat is used as a nega

10、tive control and received intraperitonealinjections of glucose solution. After the 6th injection, the two rats are sacrified; blood and perilymphatic fluidsare collected for analysis 4.Mice: Non-inbred Oncins France 1 (OF1) mice are used in the study. Ganciclovir is diluted in 5% glucoseserum to a c

11、oncentration of 5 mg/mL and administered intraperitoneally in newborn mice at a dose of 50mg/kg twice a day. Five injections are administered in total 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Brain Behav Immun. 2019 Apr 5. J Virol.

12、2017 Jan 18;91(3). pii: e02152-16. Eur J Pharm Sci. 2019 Jan 15;127:29-37.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemESee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Maggs DJ, et al. In vitro efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyc

13、lovir against feline herpesvirustype-1. Am J Vet Res. 2004 Apr;65(4):399-403.2. Fletcher CV, et al. Evaluation of ganciclovir for cytomegalovirus disease. DICP. 1989 Jan;23(1):5-12.3. Matthews T, et al. Antiviral activity and mechanism of action of ganciclovir. Rev Infect Dis. 1988 Jul-Aug;10 Suppl 3:S490-4.4. BoujemLa I, et al. Pharmacokinetics and tissue diffusion of ganciclovir in mice and rats. Antiviral Res. 2016 Aug;132:111-5.