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品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D +17 to +25, c = 1.0 in chloroform-d
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
InChI
1S/C21H25ClO6.C3H8O2.H2O/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(24)17(11-23)28-21;1-3(5)2-4;/h3-8,10,17-21,23-26H,2,9,11H2,1H3;3-5H,2H2,1H3;1H2/t17-,18-,19+,20-,21+;3-;/m10./s1
InChI 密鑰
GOADIQFWSVMMRJ-UPGAGZFNSA-N
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生化/生理作用
达格列净(BMS-512148)是一种口服活性、有效和选择性的肾钠依赖性葡萄糖共转运蛋白2(SGLT2;SLC5A2)抑制剂(人/大鼠SGLT2 IC50 = 1.1/3 nM,而人/大鼠SGLT1 IC50 = 1.39/0.6 μM;R-甲基-D-吡喃葡萄糖苷(AMG)摄取测定以及相应的CHO转染子)。达格列净通过防止肾脏葡萄糖重吸收过程并促进尿液中葡萄糖排泄,具有良好的药代动力学特性和口服利用度(口服1 mg/kg和6.6 mg/kg后,在大鼠和狗中分别降低了84%和83%),从而降低了血糖水平(在链脲佐菌素(STZ)诱导的高血糖大鼠中,在口服0.1 mg/kg后5小时降低了55%)体内。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Dapagliflozin - a breakthrough in the search for drugs to treat HFrEF.
Nature reviews. Cardiology, 16(12), 700-700 (2019-10-04)
Journal of medicinal chemistry, 51(5), 1145-1149 (2008-02-12)
The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME
Obesity research & clinical practice, 13(5), 505-510 (2019-08-31)
Chronopharmacology is the study of the varying responses of drugs to changes in biological timing and endogenous periodicities. The selective sodium-glucose cotransporter 2 inhibitor, dapagliflozin, is a globally prescribed antihyperglycemic drug. Although dapagliflozin is usually administered once a day, the
Scientific reports, 9(1), 9887-9887 (2019-07-10)
The new type 2 diabetes drug, dapagliflozin, reduces blood glucose levels and body weight by inhibiting sodium glucose transporter 2 (SGLT2) in proximal tubular cells. SGLT2 inhibitors might modulate glucose influx into renal tubular cells, thereby regulating the metabolic conditions
Metabolism: clinical and experimental, 98, 27-36 (2019-06-17)
To explore the beneficial effects of dapagliflozin and/or insulin glargine on the pancreatic beta cell mass and hepatic steatosis in db/db mice. Six-week-old db/db mice were assigned to one of four groups: untreated (Placebo), treated with dapagliflozin (Dapa), treated with
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