Canagliflozin 是SGLT2的选择性抑制剂，在表达 mSGLT2，rSGLT2 和 hSGLT2 的 CHO细胞上，IC50分别为 2 nM，3.7 nM 和 4.4 nM。

Canagliflozin, a sodium-glucose transporter 2( SGLT2) and P-Glycoprotein inhibitor, is used in type 2 diabetes.

在高糖高脂肪饲料喂养的KK小鼠中,单独口服 Canagliflozin（3 mg/kg）具有明显的抗高血糖效果.在雄性SD大鼠中,口服 Canagliflozin（30 mg/kg）能够诱导葡萄糖外排,降低血糖水平.

在注射SGLT3-的卵母细胞中,Canagliflozin（10 μM）能够抑制DNJ诱导的电流。在CHO-hSGLT1细胞（IC50=0.7 μM） 和mSGLT1 细胞（IC50=>1 μM）中,Canagliflozin抑制 14C-AMG 吸收。在L6成肌细胞中,Canagliflozin抑制(非-Na+-关联的) GLUT调节的2H-2-DG吸收。

Cells from the rat skeletal muscle cell line, L6, is used to test the effect of Canagliflozin on glucose transporter 1 (GLUT1) activity. Cells are maintained in Dulbecco's modified Eagle's medium containing 5.6 mM glucose supplemented with 10% fetal bovine serum, are seeded in 24-well plates at a density of 3 × 105 cells/well and cultured for 24 hours in an atmosphere of 5% CO2 at 37 °C. Cells are rinsed twice with Kreb's ringer phosphate HEPES buffer (pH 7.4, 150 mM NaCl, 5 mM KCl, 1.25 mM MgSO4, 1.25 mM CaCl2, 2.9 mM Na2HPO4, 10 mM HEPES) and are pre-incubated with the solutions of Canagliflozin (250 μL, 10 μM) for 5 minutes at room temperature. The transport reaction is initiated by adding 50 μL of 4.5 mM 2-DG (a substrate for GLUTs)/3H-2-DG (0.625 μCi) followed by incubation for 15 minutes at room temperature. The 2-DG uptake is halted by aspiration of the incubation mixture. Cells are immediately washed 3 times with ice-cold PBS. Samples are extracted with 0.3 N NaOH, and radioactivity is determined by liquid scintillation.(Only for Reference)

842133-18-0

C24H25FO5S

444.52

卡格列净;JNJ 28431754AAA;JNJ 28431754;JNJ 24831754ZAE;TA 7284

DMSO:82 mg/mL (184.5 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years