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Valganciclovir HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Valganciclovir HCl图片
CAS NO:175865-59-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)390.82
FormulaC14H22N6O5.HCl
CAS No.175865-59-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 78 mg/mL (199.6 mM)
Water: 78 mg/mL (199.6 mM)
Ethanol: <1 mg/mL
Other info

Chemical Name: [2-[(2-amino-6-oxo-3H-purin-9-yl)methoxy]-3-hydroxypropyl] (2S)-2-amino-3-methylbutanoate hydrochloride

InChi Key: ZORWARFPXPVJLW-MTFPJWTKSA-N

InChi Code: InChI=1S/C14H22N6O5.ClH/c1-7(2)9(15)13(23)24-4-8(3-21)25-6-20-5-17-10-11(20)18-14(16)19-12(10)22;/h5,7-9,21H,3-4,6,15H2,1-2H3,(H3,16,18,19,22);1H/t8?,9-;/m0./s1

SMILES Code: CC(C)[C@H](N)C(OCC(OCN1C=NC2=C1NC(N)=NC2=O)CO)=O.[H]Cl

SynonymsGanciclovir L-valyl ester, RS-79070-194, RS-079070-194, Cymeval, Valcyt, Valixa, Darilin, RS 079070-194, RO 107-9070/194, Rovalcyte, Patheon
实验参考方法
In Vitro

In vitro activity: Valganciclovir hydrochloride is a hydrochloride salt of the L-valyl ester of ganciclovir that exists as a mixture of two diastereomers. After administration, these diastereomers are rapidly converted to ganciclovir by hepatic and intestinal esterases. In cytomegalovirus (CMV)-infected cells, ganciclovir is initially phosphorylated to the monophosphate form by viral protein kinase, then it is further phosphorylated via cellular kinases to produce the triphosphate form. This triphosphate form is slowly metabolized intracellularly. The phosphorylation is dependent upon the viral kinase and occurs preferentially in virus-infected cells. The virustatic activity of ganciclovir is due to the inhibition of viral DNA synthesis by ganciclovir triphosphate. Ganciclovir triphosphate is incorporated into the DNA strand replacing many of the adenosine bases. This results in the prevention of DNA synthesis, as phosphodiester bridges can longer to be built, destabilizing the strand. Ganciclovir inhibits viral DNA polymerases more effectively than it does cellular polymerase, and chain elongation resumes when ganciclovir is removed.

In VivoAfter oral administration, intestinal and hepatic esterases hydrolyze both diastereomers to ganciclovir, which inhibits replication of the human cytomegalovirus. Valganciclovir is well absorbed from the gastrointestinal tract and the absolute bioavailability from valganciclovir tablets (following administration with food) is approximately 60%.
Animal modelNA
Formulation & DosageNA
References

J Pharm Sci. 2000 Jun;89(6):781-9; Drugs. 2005;65(6):859-78.