Ganciclovir.|82410-32-0|(更昔洛韦; BW 759; 2'-Nor-2'-deoxyguanosine)-陌孚医药/Medlife

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Ganciclovir. (Synonyms: 更昔洛韦; BW 759; 2'-Nor-2'-deoxyguanosine)

目录号: PC12933 纯度: ≥98%

CAS No. :82410-32-0

商品编号	规格	价格	会员价
PC12933-50mg	50mg	¥392.00	请登录
PC12933-250mg	250mg	¥1078.00	请登录
PC12933-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥637.00	请登录

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中文名称

Ganciclovir.

中文别名

更息洛韦;更昔洛韦;更昔洛韦水合物;迪克珠利;伐昔洛韦;更昔洛韦 EP标准品;更昔洛韦 USP标准品;更昔洛韦标准品;更昔洛韦-D5;更昔洛韦钠;更昔洛韦杂质混合 EP标准品;聚(3-癸基噻吩-2,5-二基);注射用阿奇霉素;9-(1,3-二羟基-2-丙氧甲基)鸟嘌呤;丙氧鸟苷;9-[[2-羟基-1-(羟甲基)乙氧基]甲基]鸟嘌呤水合物

英文名称

Ganciclovir

英文别名

2-Amino-9-(((1,3-dihydroxypropan-2-yl)oxy)methyl)-1H-purin-6(9H)-one;Ganciclovir;Ganciclovir Hydrate;Ganciclovir (BW B759U, BW 759, DHPG, 2'-Nor-2'-deoxyguanosine ,BIOLF-62,2'-NDG,Cytovene®, Cymevene®, Vitrasert®);2'-ndg;2'-Nor-2'-deoxyguanosine;biolf62;BW 759;bw-759;cymevan;cymevene;gancyclovir;GVC;HHEMG;2-Amino-1,9-dihydro-9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]-6H-purin-6-one;9-(1,3-Dihydroxy-2-propoxymethyl)guanine;DHPG;Ganciclovir ready made solution;9-[[2-Hydroxy-1-(hydroxymethyl)ethoxy]methyl]guanine Hydrate;2-Amino-1,9-dihydro-9-((2-hydroxy-1-(hydroxymethyl)ethoxy)methyl)-6H-purin-6-one;9-((2-Hydroxy-1-(hydroxymethyl)ethoxy)-methyl)guanine;2'-Nor-2'-deo;Cytovene;Vitrasert;Zirgan;Hydroxyacyclovir;Ganciclovirum;Virgan;Biolf 62;Ganciclovirum [Latin];BW 759U;9-[(1,3-Dihydroxy-2-propoxy)methyl]guanine;9-(1,3-DIHYDROXY-PROPOXYMETHANE)GUANINE;2-amino-9-{[(1,3-dihydroxypropan-2-yl)oxy]methyl}-6,9-dihydro-3H-purin-6-one;GA2;Cyt

Cas No.

82410-32-0

分子式

C₉H₁₃N₅O₄

分子量

255.23

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity 体外研究 against members of the herpes group and some other DNA viruses. Ganciclovir inhibits the 体外研究 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 an IC₅₀ of 5.2 μM for feline herpesvirus type-1 (FHV-1) and can diffuse into the brain.

性状

Solid

IC50 & Target[1][2]

CMV

HSV-1

HSV-2

FHV-1

5.2 μM (IC₅₀)

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Ganciclovir (1-80 mg/kg; i.h.; daily for 5 days) delays murine cytomegalovirus (MCMV)-induced wasting syndrome and mortality.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Non-inbred Oncins France 1 (OF1) mice and albino rats non-immunized for MCMV
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
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Faulds D, et al. Ganciclovir. A review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in cytomegalovirus infections. Drugs. 1990;39(4):597-638. [Information]

[2]. Maggs DJ, et al. 体外研究 efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyclovir against feline herpesvirus type-1. Am J Vet Res. 2004 Apr;65(4):399-403. [Information]

[3]. Boujemla I, et al. Pharmacokinetics and tissue diffusion of ganciclovir in mice and rats. Antiviral Res. 2016;132:111-115. [Information]

[4]. Fletcher CV, et al. Evaluation of ganciclovir for cytomegalovirus disease. DICP. 1989 Jan;23(1):5-12. [Information]

[5]. Matthews T, et al. Antiviral activity and mechanism of action of ganciclovir. Rev Infect Dis. 1988 Jul-Aug;10 Suppl 3:S490-4. [Information]

[6]. Duan J, Paris W, Kibler P, Bousquet C, Liuzzi M, Cordingley MG. Dose and duration-dependence of ganciclovir treatment against murine cytomegalovirus infection in severe combined immunodeficient mice. Antiviral Res. 1998;39(3):189-197. [Information]

溶解度数据

体外研究:

DMSO : 60 mg/mL (235.08 mM; Need ultrasonic)

H₂O : 1.67 mg/mL (6.54 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 3.33 mg/mL (13.05 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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