Valcyte

Valcyte - Names and Identifiers

Name	Valganciclovir hydrochloride
Synonyms	Valcyt Valcyte Rs 079070-194 Unii-4p3T9qf9nz VALGANCICLOVIR HCL Valganciclovir hydrochloride Valganciclovir hydrochloride hydrate L-VALINE,2-[(2-AMINO-1,6-DIHYDRO-6-OXO-9H-PURIN-9-YL)METHOXY]-3-HYDROXYPROPYLESTER,MONOHYDROCHLORIDE L-VALINE, 2-[(2-AMINO-1,6-DIHYDRO-6-OXO-9H-PURIN-9-YL)METHOXY]-3-HYDROXYPROPYL ESTER, MONOHYDROCHLORIDE L-Valine, 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester, monohydrochloride hydrate 2-[(2-amino-6-oxo-6,9-dihydro-3H-purin-9-yl)methoxy]-3-hydroxypropyl (2S)-2-amino-3-methylbutanoate hydrochloride hydrate
CAS	175865-59-5
EINECS	641-360-4
InChI	InChI=1/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
InChIKey	ZORWARFPXPVJLW-MTFPJWTKSA-N

Valcyte - Physico-chemical Properties

Molecular Formula	C14H23ClN6O5
Molar Mass	390.82
Melting Point	162-164°C
Boling Point	629.1°C at 760 mmHg
Flash Point	334.3°C
Solubility	H2O: ≥8mg/mL
Vapor Presure	1.08E-16mmHg at 25°C
Appearance	powder
Color	white to tan
Storage Condition	Keep in dark place,Inert atmosphere,2-8°C
Stability	Hygroscopic
In vitro study	Valganciclovir hydrochloride is the hydrochloride salt of the L-valyl ester of ganciclovir, which exists as a mixture of two diastereomers. After administration, these diastereomers are rapidly converted to ganciclovir by esterases in the liver and intestine. In macrophage (CMV) infected cells, ganciclovir is first phosphorylated by viral protein agent kinases to form monophosphate, and then further phosphorylated by cellular kinases to form triphosphate. The triphosphate is slowly metabolized in the cell. The phosphorylation process is dependent on viral kinases and occurs preferentially in virus-infected cells. The inhibition of viral activity by Ganciclovir is due to the inhibition of viral DNA synthesis by ganciclovir triphosphate. Ganciclovir triphosphate integrates into the DNA strand to displace many adenosine bases. This hinders DNA synthesis, and phosphodiester bonds take longer to form, thereby weakening the stability of the chain. Ganciclovir inhibits viral DNA polymerases more effectively than cellular polymerases, and when ganciclovir is removed, chain elongation resumes.
In vivo study	After oral administration, intestinal and hepatic esterases hydrolyze both diastereomers of ganciclovir simultaneously, inhibiting the replication of human macrophage virus. Valganciclovir is well absorbed from the gastrointestinal tract, and the bioavailability of valganciclovir tablets (administered after meals) is about 60%.