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Ganciclovir (2'-Nor-2'-deoxyguanosine, BW-759) is a novel and potent herpes simplex virus (HSV) inhibitor. It is a synthetic analog of 2'-deoxy-guanosineused to treat or prevent cytomegalovirus (CMV) infections. It acts by inhibiting the replication of human CMV with an IC50 value of 0.01 μM and is effective against strains of CMV from human, monkey, mouse, and guinea pig.
| ln Vitro |
Ganciclovir (BW 759) is an acyclic deoxyguanosine analog chemically similar to acyclovir but more effective against CMV. The median Ganciclovir concentration required to suppress viral replication by 50% is 2.15 μM, compared to 72 μM for acyclovir [4]. Ganciclovir's major mechanism of action against CMV is suppression of viral DNA replication via ganciclovir-5'-triphosphate (ganciclovir-TP). This inhibition involves the specific and strong inhibition of viral DNA polymerase. Ganciclovir is predominantly converted to its triphosphate form by three cellular enzymes: a deoxyguanosine kinase produced by CMV-infected cells, guanylate kinase, and phosphoglycerate kinase[5].
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| ln Vivo |
Ganciclovir (BW 759) (50 mg/kg; intraperitoneal; twice daily for five injections) can diffuse into the brain and the perilymphatic area of the inner ear and dramatically reduces white blood cells, red blood cells, and platelets in newborn mice[3]. Morbidity and wasting syndrome caused by the murine cytomegalovirus (MCMV) are postponed by ganciclovir (1–80 mg/kg; ih; daily for 5 days)[6].
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| Animal Protocol |
Animal/Disease Models: Non-inbred Oncins France 1 (OF1) mice and albino rats non-immunized for MCMV[3]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip)injection, twice a day for five injections (mice) or 3 days (adult rats) (pharmacokinetic/PK Study) Experimental Results: 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 demonstrated 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. Dramatically diminished white blood cells, red blood cells and platelets in newborn mice. Animal/Disease Models: Female SCID (severe combined immunodeficient) mouse inoculated with MCMV[6] Doses: 0, 1, 10, 80 and 160 mg/kg Route of Administration: subcutaneous (sc) injection, one time/day for 5 days Experimental Results: Dose dependently delayed the wasting syndrome and mortality in a dose |
| References |
[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.
[2]. 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. [3]. Boujemla I, et al. Pharmacokinetics and tissue diffusion of ganciclovir in mice and rats. Antiviral Res. 2016;132:111-115. [4]. Fletcher CV, et al. Evaluation of ganciclovir for cytomegalovirus disease. DICP. 1989 Jan;23(1):5-12. [5]. Matthews T, et al. 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. |
| Molecular Formula |
C9H13N5O4
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|---|---|
| Molecular Weight |
255.23
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| Exact Mass |
255.0968
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| Elemental Analysis |
C, 42.35; H, 5.13; N, 27.44; O, 25.07
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| CAS # |
82410-32-0
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| Related CAS # |
Ganciclovir sodium;107910-75-8;Ganciclovir-d5;1189966-73-1;Ganciclovir hydrate;1359968-33-4
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| Appearance |
Solid powder
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| SMILES |
O=C(N=C(N)N1)C2=C1N(C=N2)COC(CO)CO
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| InChi Key |
IRSCQMHQWWYFCW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13N5O4/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)
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| Chemical Name |
2-amino-1,9-dihydro-9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]-6H-purin-6-one
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| Synonyms |
2'-Nor-2'-deoxyguanosine, BW-759 BW 759
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~60 mg/mL (~235.08 mM)
H2O : ~1.67 mg/mL (~6.54 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (8.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (8.15 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 3.33 mg/mL (13.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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