更昔洛韋作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetGanciclovirCat. No.: HY-13637CAS No.: 82410-32-0分式: CHNO分量: 255.23作靶點(diǎn): HSV作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) 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(chǔ)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(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In V

3、itro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請(qǐng)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(chǔ)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(qǐng)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(chǔ)備液加到 900 L 20% 的

5、SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)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(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 30.0 mg/mL 的澄 DMSO 儲(chǔ)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(xì)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(nèi)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(chǎn)品發(fā)表的科研獻(xiàn) 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-