更昔洛韋作用機制 - Medchemexpress - MCE中國

1、Product Data SheetGanciclovirCat. No.: HY-13637CAS No.: 82410-32-0分式: CHNO分量: 255.23作靶點: HSV作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 60 mg/mL (235.08 mM; Need ultrasonic)H2O : 3.67 mg/mL (14.38 mM; Need ultrasonic)SolventMass1 mg 5 mg

2、10 mgConcentration制備儲備液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請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In V

3、itro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (11.75 mM); Clear solution此案可獲得 3 mg/mL (11.75 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 30.0 m

4、g/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (11.75 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 3 mg/mL (11.75 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 30.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的

5、SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (11.75 mM); Clear solution此案可獲得 3 mg/mL (11.75 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 30.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Ganciclovir是有效的單純皰疹病毒 (HSV) 抑制劑，包括巨細胞病毒（CMV），抑制FHV-1的 IC50 值為5.

6、2 M 。IC & Target IC50: 5.2 M (FHV-1)1體外研究 Ganciclovir is an acyclic deoxyguanosine analog structurally similar to acyclovir but with superior activity against CMV.The median ganciclovir concentration required to inhibit viral replication by 50 percent is 2.15 mumol versus 72mumol for acyclovir2.The

7、primary mechanism of ganciclovir action against CMV is inhibition of the replication ofviral DNA by ganciclovir-5-triphosphate (ganciclovir-TP). This inhibition includes a selective and potent inhibition ofthe viral DNA polymerase.Ganciclovir is metabolized to the triphosphate form by primarily thre

8、e cellular enzymes: adeoxyguanosine kinase induced by CMV-infected cells; guanylate kinase; and phosphoglycerate kinase3.體內研究 In adult rats, the intracochlear diffusion of ganciclovir is shown to achieve the same concentration as in blood. Ingestating mice, transplacental diffusion is observed, with

9、 a fetal-to-maternal blood ratio of 0.5. In newborn mice, theplasma concentration profile of ganciclovir shows a peak at 2 h followed by a gradual decrease. In adult mice, theconcentration peaked at 1 h, but becomes undetectable by 2 h after injection. Counts of white blood cells, red bloodcells and

10、 platelets decreases significantly in ganciclovir-treated newborn mice4.PROTOCOLAnimal Rats: Two albino rats non-immunized for MCMV are used in the study. After being weighed, two adult rats undergoAdministration 4 peritoneal injections. The first rat receives 50 mg/kg of ganciclovir twice a day (i.

11、e. 100 mg/kg/day), for a total of 3days or 6 injections. The second rat is used as a negative control and received intraperitoneal injections of glucosesolution. After the 6th injection, the two rats are sacrified; blood and perilymphatic fluids are collected for analysis4.Mice: Non-inbred Oncins Fr

12、ance 1 (OF1) mice are used in the study. Ganciclovir is diluted in 5% glucose serum to aconcentration of 5 mg/mL and administered intraperitoneally in newborn mice at a dose of 50 mg/kg twice a day.Five injections are administered in total4.MCE has not independently confirmed the accuracy of these m

13、ethods. They are for reference only.戶使本產品發(fā)表的科研獻 Brain Behav Immun. 2019 Aug;80:394-405. J Virol. 2017 Jan 18;91(3). pii: e02152-16. Eur J Pharm Sci. 2019 Jan 15;127:29-37.Page 2 of 3 www.MedChemE Pharmacol Res Perspect. 2020 Apr;8(2):e00575. bioRxiv. 2019 Oct.See more customer validations on HYPERLI

14、NK www.MedChemE www.MedChemEREFERENCES1. Maggs DJ, et al. In vitro efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyclovir against feline herpesvirus type-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-