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Merck
CN

SML4200

Empagliflozin

≥98% (HPLC)

别名:

1-Chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yl-oxy)-benzyl]-benzene, (1S)-1,5-Anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-D-glucitol, (2S,3R,4R,5S,6R)-2-(4-Chloro-3-(4-((S)-tetrahydrofuran-3-yloxy]benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, BI 10773, BI-10773, BI10773

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关于此项目

经验公式（希尔记法）:
C23H27ClO7
化学文摘社编号:
864070-44-0
分子量:
450.91
MDL number:
MFCD22566222
NACRES:
NA.21
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
100

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assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Quality Level

100

General description

Empagliflozin is a C-glucoside with a carbon-carbon bond between the glucose and aglycone, resisting the breakdown in the gastrointestinal tract.

Application

Empagliflozin may be used to study its effects on diabetes mellitus in animal models.

Biochem/physiol Actions

Empagliflozin (BI 10773) is an orally active, potent and highly selective sodium glucose co-transporter-2 inhibitor (hSGLT-2 IC50 = 3.1 nM; hSGLT-1/4/5/6 IC50 = 8.3/11/1.1/2.0 µM) that targets SGLT-2 with high affinity in a glucose-competitive manner (hSGLT-2 Kd = 57/194 nM in the absence/presence of 20 mM glucose). Empagliflozin improves glycaemic control in type 2 (1-3 mg/kg via daily p.o. to Zucker diabetic fatty (ZDF) rats) and type 1 (10 mg/kg b.i.d. p.o. to streptozotocin-induced diabetic (STD) rats) diabetes mellitus models.

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分析证书(COA)

Lot/Batch Number
0000514190
0000514192
0000514192
0000514190
0000505557

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R Grempler et al.
Diabetes, obesity & metabolism, 14(1), 83-90 (2011-10-12)
Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor in clinical development for the treatment of type 2 diabetes mellitus. This study assessed pharmacological properties of empagliflozin in vitro and pharmacokinetic properties in vivo and compared its potency and selectivity
L Thomas et al.
Diabetes, obesity & metabolism, 14(1), 94-96 (2011-10-12)
Empagliflozin is a potent, selective sodium glucose co-transporter-2 inhibitor that is in development for the treatment of type 2 diabetes. This series of studies was conducted to assess the in vivo pharmacological effects of single or multiple doses of empagliflozin
G Luippold et al.
Diabetes, obesity & metabolism, 14(7), 601-607 (2012-01-25)
Sodium glucose cotransporter-2 (SGLT-2) is key to reabsorption of glucose in the kidney. SGLT-2 inhibitors are in clinical development for treatment of type 2 diabetes mellitus (T2DM). The mechanism may be of value also in the treatment of type 1

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