中文名 | 坎格列净 |
英文名 | canagliflozin |
别名 | 坎格列净 卡格列净 卡格列净半水 卡格列净半水物 坎格列嗪半水物 卡格列净无水物 卡格列净半水合物 坎格列净(半水) 坎格列净半水合物 坎格列净半水化合物 坎格列净半水合物(坎格列净) (1S)-1,5-脱氢-1-C-[3-[[5-(4-氟苯基)-2-噻吩基]甲基]-4-甲基苯基]-D-葡萄糖醇 |
英文别名 | Cageline canagliflozin Cagliflozin heMihydrate Canagliflozin heMihydrate Canagliflozin heMihydrates 1-(β-D-glucopyranosyl)-4-methyl-3-(5-(4-fluorophenyl)-2-thienyl-methyl) benzene (1s)-1,5-anhydro-1-c-(3-((5-(4-fluorophenyl)-2-thienyl)methyl)-4-methylphenyl)-d-glucitol (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol Hemihydrate |
CAS | 842133-18-0 928672-86-0 |
EINECS | 202-303-5 |
化学式 | 2(C24H25FO5S).H2O |
分子量 | 462.53 |
密度 | 1.4±0.1 g/cm3 |
熔点 | 94-96°C |
沸点 | 642.9±55.0 °C at 760 mmHg |
闪点 | 342.6±31.5 °C |
溶解度 | DMSO (微溶) 、甲醇 (微溶) |
存储条件 | Hygroscopic, Refrigerator, under inert atmosphere |
稳定性 | 吸湿性 |
外观 | 固体 |
颜色 | White to Off-White |
MDL号 | MFCD18251436 |
体外研究 | Canagliflozin inhibits Na + -dependent 14 C-AMG uptake in CHO-hSGLT2 cells, with an IC 50 of 4.4±1.2 nM. Similar IC 50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC 50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14 C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC 50 of 684±159 nM and >1,000 nM, respectively. |
体内研究 | Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats. Animal Model: Diet-induced obese, insulin resistantmice (DIO) Mice Dosage: 30 mg/kg Administration: Oral gavage; daily; 4 weeks Result: Reduced BG levels, respiratory exchange ratio, and body weight gain. Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats Dosage: 3 mg/kg Administration: Oral gavage; daily; 3 weeks Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight. |
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