Ganciclovir (BW 759) 是一种核苷类似物和口服抗病毒药物，对CMV具有抗病毒活性。Ganciclovir 在体外对疱疹病毒 (herpes group) 和其他一些 DNA 病毒也具有抗病毒活性。Ganciclovir 抑制人类疱疹病毒 (HSV 1 型和 2 型，CMV) 和腺病毒血清型1、2、4、6、8、10、19、22 和 28 的体外复制。Ganciclovir 对猫 1 型疱疹病毒 (FHV-1) 的IC50为 5.2 μM，可透过大脑屏障。
| 生物活性 | Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity againstCMV. Ganciclovir also has activity in vitro against members of theherpes groupand some other DNA viruses. Ganciclovir inhibits the in vitro replication of human herpes viruses (HSV 1 and 2, CMV) and adenovirus serotypes 1, 2, 4, 6, 8, 10, 19, 22 and 28. Ganciclovir has anIC50of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain[1][2][3]. |
| IC50& Target[1][2][3] | CMV | HSV-1 | HSV-2 | FHV-1 5.2 μM (IC50) |
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体外研究
(In Vitro) | Ganciclovir (BW 759) 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 μM versus 72 μM for acyclovir[4].
The primary mechanism of Ganciclovir action against CMV is inhibition of the replication of viral DNA by ganciclovir-5'-triphosphate (ganciclovir-TP). This inhibition includes a selective and potent inhibition of the viral DNA polymerase. Ganciclovir is metabolized to the triphosphate form by primarily three cellular enzymes: a deoxyguanosine kinase induced by CMV-infected cells; guanylate kinase; and phosphoglycerate kinase[5].
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体内研究
(In Vivo) | Ganciclovir (BW 759) (50 mg/kg; i.p.; twice a day for five injections) significantly decreases white blood cells, red blood cells and platelets in newborn mice, and can diffuse into the brain and the perilymphatic space of the inner ear[3].
Ganciclovir (1-80 mg/kg; i.h.; daily for 5 days) delays murine cytomegalovirus (MCMV)-induced wasting syndrome and mortality[6].
| Animal Model: | Non-inbred Oncins France 1 (OF1) mice and albino rats non-immunized for
MCMV[3] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection, twice a day for five injections (mice) or 3 days (adult rats) (Pharmacokinetic Study) | | Result: | In adult rats, the intracochlear diffusion of Ganciclovir was shown to achieve the same concentration as in blood. In gestating mice, transplacental diffusion was observed, with a fetal-to-maternal blood ratio of 0.5. In newborn mice, the plasma concentration profile of Ganciclovir showed a peak at 2 h followed by a gradual decrease. In adult mice, the concentration peaked at 1 h, but became undetectable by 2 h after injection.
Significantly decreased white blood cells, red blood cells and platelets in newborn mice. |
| Animal Model: | Female SCID mice inoculated with MCMV[6] | | Dosage: | 0, 1, 10, 80 and 160 mg/kg | | Administration: | Subcutaneous injection, once daily for 5 days | | Result: | Dose dependently delayed the wasting syndrome and mortality in a dose range up to 80 mg/kg per day, whereas a dose of 160 mg/kg per day induced reversible side-effects. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 60 mg/mL(235.08 mM;Need ultrasonic) H2O : 1.67 mg/mL(6.54 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.9180 mL | 19.5902 mL | 39.1803 mL | | 5 mM | 0.7836 mL | 3.9180 mL | 7.8361 mL | | 10 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；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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 3.33 mg/mL (13.05 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (8.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (8.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (8.15 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (8.15 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (8.15 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (8.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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