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[CAS NO. 1359968-33-4]  Ganciclovir hydrate

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PRODUCTS SPECIFICATIONS [1359968-33-4]

Catalog
HY-13637B
Brand
MCE
CAS
1359968-33-4

DESCRIPTION [1359968-33-4]

Overview

MDL-
Molecular Weight273.25
Molecular FormulaC9H15N5O5
SMILESO=C1N=C(NC2=C1N=CN2COC(CO)CO)N.O

For research use only. We do not sell to patients.

11 Publications Citing Use of MCE


Summary

Ganciclovir (BW 759) hydrate, a nucleoside analogue, is an orally active antiviral agent with activity against CMV . Ganciclovir hydrate also has activity in vitro against members of the herpes group and some other DNA viruses. Ganciclovir hydrate 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 hydrate has an IC 50 of 5.2 μM for feline herpesvirus type-1 ( FHV-1 ) and can diffuse into the brain [1] [2] [3] .


IC50 & Target

CMV

HSV-1

HSV-2

FHV-1

5.2 μM (IC 50 )


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] .

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


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] .

MCE 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 [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.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00001062 National Institute of Allergy and Infectious Diseases (NIAID)
Cytomegalovirus Retinitis|HIV Infections
Phase 1
NCT00000143 Johns Hopkins Bloomberg School of Public Health
Cytomegalovirus Retinitis|HIV Infections
May 1997 Phase 3
NCT03217474 Chunxiao Wang|Sun Yat-sen University
Herpes Simplex Keratitis
July 20, 2017 Not Applicable

Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Please store the product under the recommended conditions in the Certificate of Analysis.



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