Ganciclovir (BW 759), a nucleoside analogue, is an orally active antiviral agent with activity against CMV. Ganciclovir also has activity in vitro against members of the herpes group and 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 an IC50 of 5.2 μM for feline herpesvirus type-1 (FHV-1).
体外研究
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 mumol versus 72 mumol 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.
体内研究
Ganciclovir (BW 759) (1-80 mg/kg; i.h.; daily for 5 days) delays murine cytomegalovirus (MCMV)-induced wasting syndrome and mortality.
Animal Model:
Severe combined immunodeficiency (SCID) mice (MCMV infection)
Dosage:
1-80 mg/kg
Administration:
I.h.; daily for 5 days
Result:
Dose dependently delayed MCMV-induced wasting syndrome and mortality.
分子式
C9H13N5O4
分子量
255.23
CAS号
82410-32-0
中文名称
更昔洛韦;更息洛韦;丙氧鸟苷
运输条件
Room temperature in continental US; may vary elsewhere.