详细介绍
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
cagliflozinhemihydrate
canagliflozinhemihydrate
canagliflozinhemihydrates
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-triolhemihydrate
cas842133-18-0
928672-86-0
einecs202-303-5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 (slightly), methanol (slightly)存储条件hygroscopic, refrigerator, under inert atmosphere稳定性hygroscopic外观solid颜色white to off-whitemdl号mfcd18251436体外研究canagliflozin inhibits na + -dependent 14 c-amg uptake incho-hsglt2 cells, with an ic 50 of 4.4±1.2 nm. similar ic 50 valuesare obtained in cho-rsglt2 and cho-msglt2 cells (ic 50 = 3.7 and2.0 nm for rat and mouse sglt2, respectively). canagliflozininhibits 14 c-amg uptake in cho-hsglt1 and msglt1 cells with ic 50of 684±159 nm and >1,000 nm, respectively.体内研究canagliflozin (30 mg/kg treatment for 4 weeks) reduced bloodglucose (bg) levels, respiratory exchange ratio, and body weightgain in dio mice. canagliflozin (3 mg/kg for 3 weeks) increasesurinary glucose excretion (uge) with no significant change in totalfood intake compared with that in vehicle-treated rats, leading toa decrease in body weight in zf rats. animal model: diet-inducedobese, insulin resistantmice (dio) mice dosage: 30 mg/kgadministration: oral gavage; daily; 4 weeks result: reduced bglevels, respiratory exchange ratio, and body weight gain. animalmodel: male zucker fatty (zf) obese, insulin resistant rats dosage:3 mg/kg administration: oral gavage; daily; 3 weeks result: uge wasincreased with no significant change in total food intake comparedwith that in vehicle-treated rats, leading to a decrease in bodyweight.
医药中间体
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