Ganciclovir是一种核苷类抗病毒药物。
Cas No.:82410-32-0
Sample solution is provided at 25 µL, 10mM.
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Ganciclovir is a nucleoside antiviral drug. Ganciclovir enters cells and is phosphorylated to a triphosphate compound, which competitively inhibits DNA polymerase and incorporates into viral DNA, thereby inhibiting DNA synthesis. Ganciclovir can be used for the treatment of cytomegalovirus retinitis in immunocompromised patients (including AIDS patients) and for the prevention of cytomegalovirus infection in organ transplant recipients[1-4].
In vitro, B lymphoblastoid cells were treated with Ganciclovir (1-20μg/ml) for 1-14 days. When the exposure duration exceeded 2 days, the dose of Ganciclovir was positively correlated with cytotoxicity, and the cytotoxic concentration significantly decreased with prolonged exposure time[5]. Microglial cells were treated with Ganciclovir (0.05–1mM) for 48 hours. In the presence or absence of LPS (100ng/ml), Ganciclovir did not significantly affect cell proliferation or viability[6].
In vivo, BALB/c mice were intraperitoneally injected daily with Ganciclovir (25–40mg/kg/day), starting from day 1 after infection with murine cytomegalovirus (MCMV) and continuing until day 7. Ganciclovir significantly reduced the occurrence of acute-phase myocarditis in mice[7]. BALB/c mice infected with MCMV on postnatal day 3 were intraperitoneally injected twice daily with Ganciclovir (10mg/kg) for 14 days. Ganciclovir significantly reduced the viral load in the temporal bones of mice, alleviated MCMV-induced sensorineural hearing loss, and partially protected against outer hair cell loss[8].
References:
[1] Crumpacker CS. Ganciclovir. N Engl J Med. 1996 Sep 5;335(10):721-9.
[2] Al-Badr AA, Ajarim TDS. Ganciclovir. Profiles Drug Subst Excip Relat Methodol. 2018;43:1-208.
[3] Ernst ME, Franey RJ. Acyclovir- and ganciclovir-induced neurotoxicity. Ann Pharmacother. 1998 Jan;32(1):111-3.
[4] McGavin JK, Goa KL. Ganciclovir: an update of its use in the prevention of cytomegalovirus infection and disease in transplant recipients. Drugs. 2001;61(8):1153-83.
[5] Janoly-Dumenil A, Rouvet I, Bleyzac N, et al. Effect of duration and intensity of ganciclovir exposure on lymphoblastoid cell toxicity. Antivir Chem Chemother. 2009;19(6):257-62.
[6] Skripuletz T, Salinas Tejedor L, Prajeeth CK, et al. The antiviral drug ganciclovir does not inhibit microglial proliferation and activation. Sci Rep. 2015 Oct 8;5:14935.
[7] Lenzo JC, Shellam GR, Lawson CM. Ganciclovir and cidofovir treatment of cytomegalovirus-induced myocarditis in mice. Antimicrob Agents Chemother. 2001 May;45(5):1444-9.
[8] Haller TJ, Price MS, Lindsay SR, et al. Effects of ganciclovir treatment in a murine model of cytomegalovirus-induced hearing loss. Laryngoscope. 2020 Apr;130(4):1064-1069.
Ganciclovir是一种核苷类抗病毒药物。Ganciclovir进入细胞后被磷酸化为三磷酸化合物，竞争性抑制DNA多聚酶并掺入病毒DNA中从而抑制DNA合成。Ganciclovir可用于免疫缺陷患者（包括艾滋病患者）的巨细胞病毒性视网膜炎治疗和器官移植受者的巨细胞病毒感染预防[1-4]。
在体外，Ganciclovir（1-20μg/ml）处理B淋巴母细胞1-14天。当暴露时间超过2天时，Ganciclovir的剂量与细胞毒性呈正相关，同时细胞毒性浓度随暴露时间延长而显著降低[5]。Ganciclovir（0.05–1mM）处理小胶质细胞48小时。在存在或不存在LPS（100ng/ml）的情况下，Ganciclovir没有显著影响细胞增殖或活力 [6]。
在体内，Ganciclovir（25–40mg/kg/day）每日腹腔注射于BALB/c小鼠，从感染鼠巨细胞病毒（MCMV）后第1天开始，持续到第7天。Ganciclovir显著减少了小鼠急性期心肌炎的发生[7]。Ganciclovir（10mg/kg）每日两次腹腔注射于出生后第3天感染MCMV的BALB/c小鼠，持续14天。Ganciclovir显著降低了小鼠颞骨内的病毒载量，减轻了MCMV诱导的感音神经性听力损失，并部分保护了外毛细胞损失[8]。
| Cell experiment [1]: | |
Cell lines | B lymphoblastoid cells (BLCLs) by infection with Epstein-Barr virus. |
Preparation Method | BLCLs were grown as suspension cultures in RPMI 1640 medium supplemented with 12% fetal bovine serum, penicillin (120UI/ml), streptomycin (120μg/ml) and amphotericin B (1μg/ml) at 37°C in a humidified atmosphere of 5% CO₂. BLCLs were treated with Ganciclovir (1-20μg/ml). |
Reaction Conditions | 1-20μg/ml; 1-14 days. |
Applications | Ganciclovir exposure was associated with cell toxicity and decreased growth at days 7 and 14 for all concentrations and incubation periods. The 50% cytotoxic concentrations (CC₅₀) markedly decreased with the duration of Ganciclovir exposure from 374μg/ml (for 1-day exposure) to 3.0μg/ml (for 14-day exposure). Microscopic examination indicated an alteration and decrease in cell clusters associated with high Ganciclovir concentration (20μg/ml). |
| Animal experiment [2]: | |
Animal models | BALB/c mice (6 to 8 weeks old) |
Preparation Method | Mice were infected intraperitoneally with 105 PFU of MCMV (K181 strain) on day 0. Ganciclovir treatment commenced on day 1 postinfection and continued daily. |
Dosage form | 25-40mg/kg/day; i.p.; daily injection for 7 days. |
Applications | Ganciclovir treatment significantly reduced the acute phase of myocarditis (6.2-fold reduction) on day 7 postinfection in MCMV-infected mice. |
References: | |
| Cas No. | 82410-32-0 | SDF | |
| 别名 | 更昔洛韦; BW 759; 2'-Nor-2'-deoxyguanosine | ||
| 化学名 | 2-amino-9-(1,3-dihydroxypropan-2-yloxymethyl)-3H-purin-6-one | ||
| Canonical SMILES | C1=NC2=C(N1COC(CO)CO)NC(=NC2=O)N | ||
| 分子式 | C9H13N5O4 | 分子量 | 255.23 |
| 溶解度 | >50mg/mL in DMSO (Need ultrasonic) | 储存条件 | Store at 2-8°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.918 mL | 19.5902 mL | 39.1803 mL |
| 5 mM | 783.6 μL | 3.918 mL | 7.8361 mL |
| 10 mM | 391.8 μL | 1.959 mL | 3.918 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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