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Rosiglitazone

Rosiglitazone ??? ???
?? ??:
122320-73-4
???:
Rosiglitazone
???(??):
AVANDIA;ROSIGLITAZONE HCL;Rosig;RosigL;itazone;BRL 49653;50MG/1G/1KG;ROSIGLIAZONE;roiglitazone;ROSIGLITAZONE
CBNumber:
CB7133275
???:
C18H19N3O3S
??? ??:
357.43
MOL ??:
122320-73-4.mol
MSDS ??:
SDS

Rosiglitazone ??

???
153-155 C
?? ?
585.0±35.0 °C(Predicted)
??
1.315±0.06 g/cm3(Predicted)
?? ??
2-8°C
???
DMSO: ≥10mg/mL
?? ?? (pKa)
6.34±0.50(Predicted)
??? ??
??
??
???? ?????
Merck
14,8265
CAS ??????
122320-73-4(CAS DataBase Reference)
IARC
3 (Vol. 108) 2016
??
  • ?? ? ?? ??
  • ?? ? ???? ?? (GHS)
??? ?? Xi
?? ???? ?? 36/38
????? 26-37/39
WGK ?? 3
RTECS ?? XJ5813850
HS ?? 2934100000
?? ?? ??? 122320-73-4(Hazardous Substances Data)
????(GHS): GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
?? ?: Warning
??·?? ??:
?? ??·?? ?? ?? ?? ?? ?? ? ?? ?? P- ??
H319 ?? ?? ??? ??? ?? ? ?? ?? ??? ?? ?? 2A ?? GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H361 ?? ?? ????? ??? ??? ??? ??? ???? ?? ?? 2 ?? P201, P202, P281, P308+P313, P405,P501
H410 ??? ??? ?? ????? ?? ??? ?? ????? ?? - ?? ?? 1 ?? GHS hazard pictograms P273, P391, P501
??????:
P201 ?? ? ?? ???? ?????.
P202 ?? ?? ?? ??? ?? ???? ??? ???? ???.
P264 ?? ??? ?? ??? ????.
P264 ?? ??? ?? ??? ????.
P273 ???? ???? ???.
P280 ????/???/???/?????? ?????.
P281 ???? ?? ???? ?????
P305+P351+P338 ?? ??? ? ?? ?? ???? ????. ???? ?????? ?????. ?? ????.
P308+P313 ?? ?? ??? ???? ???? ??· ??? ????.
P391 ???? ????.
P405 ???? ?????.
P501 ...? ??? / ??? ?? ???.
NFPA 704
0
2 0

Rosiglitazone C??? ??, ??, ??

??

Rosiglitazone is an insulin sensitizer; binds to peroxisome proliferator activated receptor gamma (PPAR- γ).

Indications

Rosiglitazone is approved for use as monotherapy and in conjunction with metformin, though it is sometimes combined with a sulfonylurea or insulin. It is usually taken once or twice a day with or without food. Rosiglitazone may cause a modest increase in lowdensity lipoprotein and triglyceride concentrations, but it is unclear whether this effect has any clinical significance or persists in the long term.

?? ??

Rosiglitazone is 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, and is availableas the maleate salt in tablets containing the drug alone(Avandia) or in combination products with metformin(Avandamet) or with glimepiride (Avandaryl). The2-aminopyridine moiety allows for salt formation; the marketedformulations contain the 1:1 salt with maleic acid, inwhich the pyridine nitrogen accepts a proton, forming the2-aminopyridinium species.

Clinical Use

Although rosiglitazone is extensively biotransformed—playing the major role in both transformations, and some involvementof CYP2C9.21,47 The sulfate conjugate M10 is thepredominant circulating metabolite by 4-hour postdose. Theextraordinarily high plasma protein binding of this metabolite(and the N-demethylated sulfate conjugate M4) in humans accountsfor the lengthy residence time of the radioactivity in thebody, despite the relatively short pharmacokinetic half-life(4–4.5 hours) of rosiglitazone itself.

Rosiglitazone ?? ?? ? ???

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Rosiglitazone ?? ??

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Rosiglitazone ?? ??:

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