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Entecavir

Entecavir ??? ???
?? ??:
142217-69-4
???:
Entecavir
???(??):
Etv;Baraclude;entikawei;2-amino-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-1H-purin-6(9H)-one;CS-863;CS-1236;Entecavi;SQ 34676;Enticavir;ENTECAVIR
CBNumber:
CB0506719
???:
C12H15N5O3
??? ??:
277.28
MOL ??:
142217-69-4.mol

Entecavir ??

???
249-252°C
?? ?
661.4±65.0 °C(Predicted)
??
1.81±0.1 g/cm3(Predicted)
?? ??
-20°C
???
DMSO(?? ???), ???(?? ???)
?? ?? (pKa)
14.22±0.60(Predicted)
??? ??
??
??
???? ????
optical activity
[α]/D +25 to +40°, c = 0.2 in H2O
???
H2O: 0.5mg/mL, clear (warmed)
???
???
CAS ??????
142217-69-4(CAS DataBase Reference)
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
????? 24/25
WGK ?? 3
HS ?? 29339900
?? ?? ??? 142217-69-4(Hazardous Substances Data)
????(GHS): GHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H302 ??? ??? ?? ?? ?? - ?? ?? 4 ?? GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 ??? ??? ??? ????? ?? ????? ?? 2 ?? GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H320 ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2B ?? P264, P305+P351+P338,P337+P313
H335 ?? ???? ??? ? ?? ?? ???? ?? - 1? ??;???? ?? ?? 3 ?? GHS hazard pictograms
??????:
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P270 ? ??? ??? ??? ???, ???? ???? ???.
P301+P312 ??? ???? ??? ????(??)? ??? ????.
P330 ?? ?????.

Entecavir C??? ??, ??, ??

??

Entecavir is a cyclopentyl guanosine analog launched for the once-daily oral treatment of chronic hepatitis B virus (HBV) infection, and it is the third nucleoside or nucleotide analog to be marketed for this indication. Lamivudine, a deoxythiacytosine analog, and adefovir dipivoxil, a nucleotide analog, have been marketed since 1998 and 2002, respectively. Entecavir and adefovir are specifically indicated for HBV, whereas lamivudine is indicated for both HBV and HIV infections.

??? ??

White to Off-White/Yellow Crystalline Powder

??

ChEBI: Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it ha no activity against HIV. It is used for the treatment of chronic hepatitis B.

???

Baraclude (BMS)

Clinical Use

Treatment of chronic hepatitis B virus infection in patients >16 years of age.
Entecavir comes as a tablet and solution (liquid) to take by mouth. It is usually taken once a day on an empty stomach, at least 2 hours after a meal and at least 2 hours before the next meal. Take entecavir at around the same time every day.

Entecavir ?? ?? ? ???

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Entecavir ?? ??

???( 528)?? ??
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Entecavir ?? ??:

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