无环脱氧鸟苷类似物更昔洛韦 (BW 759) 具有很强的抗 CMV 作用，结构与阿昔洛韦类似。与阿昔洛韦的 72 μM 相比，抑制病毒繁殖 50% 所需的更昔洛韦的中位剂量为 2.15 μM [4]。更昔洛韦使用 5'-三磷酸更昔洛韦 (ganciclovir-TP)，抑制病毒 DNA 复制，这是对抗 CMV 的主要作用机制。该抑制剂可特异性、有效地抑制病毒 DNA 聚合酶。三种生物酶主要将更昔洛韦转化为其三磷酸盐形式：磷酸甘油酸激酶、鸟苷酸激酶和脱氧鸟苷激酶，它们在CMV感染的细胞中被激活[5]。

总共五次腹腔注射，更昔洛韦 (BW 759) (50 mg/kg) 显着降低新生小鼠的白细胞、红细胞和血小板。它还可以扩散到外耳和大脑。淋巴空间。 3]。在感染巨细胞病毒 (MCMV) 的小鼠中，更昔洛韦（1-80 mg/kg；静脉注射；每天一次，持续 5 天）可推迟消耗综合征和死亡率 [6]。

Animal/Disease Models: non-inbred Oncins France 1 (OF1) mice and albino rats without MCMV immunization [3]
Doses: 50 mg/kg
Route of Administration: intraperitoneal (ip) injection, twice a day, for 5 consecutive injections (mouse ) or 3 days (adult rats) ) (pharmacokinetic/PK/PK study)
Experimental Results: In adult rats, intracochlear diffusion of ganciclovir reaches the same concentration as in blood. In pregnant mice, transplacental spread was observed with a fetal to maternal blood ratio of 0.5. In neonatal mice, plasma concentrations of ganciclovir peak within 2 hrs (hrs (hours)) and gradually decrease thereafter. In adult mice, concentrations peaked at 1 hour but became undetectable at 2 hrs (hrs (hours)) post-injection. White blood cells, red blood cells and platelets were Dramatically diminished in newborn mice.

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Animal/Disease Models: Female SCID (severe combined immunodeficient) mouse vaccinated with MCMV[6] Doses: 0, 1, 10, 80 and 160 mg/kg
Route of Administration: subcutaneous injection, one time/day for 5 days
Experimental Results: Within a certain dose range, dose-dependent Delayed wasting syndrome

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

[2]. 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.

[3]. Pharmacokinetics and tissue diffusion of ganciclovir in mice and rats. Antiviral Res. 2016;132:111-115.

[4]. Evaluation of ganciclovir for cytomegalovirus disease. DICP. 1989 Jan;23(1):5-12.

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

[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.

Ganciclovir Sodium can cause developmental toxicity and male reproductive toxicity according to state or federal government labeling requirements.
Ganciclovir is an antiviral prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of cytomegalovirus retinitis (CMV retinitis) in adults who are immunocompromised, including individuals with AIDS. Ganciclovir is also FDA-approved for the prevention of CMV disease in recipients of organ transplants who are at risk for CMV diseases.
CMV diseases, including CMV retinitis, can be opportunistic infections (OIs) of HIV.
Ganciclovir Sodium is the sodium salt form of ganciclovir, a synthetic, antiviral, purine nucleoside analog with antiviral activity, especially against cytomegalovirus (CMV). Ganciclovir sodium is a prodrug that is phosphorylated and subsequently converted into its triphosphate form, the active metabolite ganciclovir-5-triphosphate (ganciclovir-TP), in the infected cells by cellular kinases. Ganciclovir-TP competes as a substrate with nucleotide triphosphates for viral DNA polymerase. Once it gets incorporated into DNA strand, it prevents further polymerization of DNA, thereby interfering with viral DNA replication.
An ACYCLOVIR analog that is a potent inhibitor of the Herpesvirus family including cytomegalovirus. Ganciclovir is used to treat complications from AIDS-associated cytomegalovirus infections.

C9H12N5NAO4

277.21

277.078

C, 38.99; H, 4.36

107910-75-8

Ganciclovir;82410-32-0;Ganciclovir hydrate;1359968-33-4

23700083

White to off-white solid powder

1.81g/cm3

675ºC at 760mmHg

250ºC (decomposition)

362ºC

142.37

3

8

5

19

273

0

C(C(CO)OCN1C=NC2=C1NC(=N)N=C2[O-])O.[Na+]

JJICLMJFIKGAAU-UHFFFAOYSA-M

InChI=1S/C9H13N5O4.Na/c10-9-12-7-6(8(17)13-9)11-3-14(7)4-18-5(1-15)2-16;/h3,5,15-16H,1-2,4H2,(H3,10,12,13,17);/q;+1/p-1

sodium;2-amino-9-(1,3-dihydroxypropan-2-yloxymethyl)purin-6-olate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: 25 mg/mL (90.18 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。