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产品名称
达格列净, ≥98% (HPLC)
质量水平
方案
≥98% (HPLC)
表单
powder
旋光性
[α]/D (+7.0° to +13.0°, c = 0.2 in methanol)
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
CCOC1=CC=C(C=C1)CC2=C(C=CC([C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)=C2)Cl
InChI
1S/C21H25ClO6/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/h3-8,10,17-21,23-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
InChI key
JVHXJTBJCFBINQ-ADAARDCZSA-N
生化/生理作用
口服活性，强效和选择性肾钠依赖性葡萄糖共转运蛋白2（SGLT2；SLC5A2）抑制剂，在体内具有降血糖功效。
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。
警示用语：
Danger
危险分类
Acute Tox. 4 Oral - Aquatic Chronic 2 - Eye Irrit. 2 - STOT RE 1
靶器官
Kidney
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Wei Meng et al.
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
Dapagliflozin - a breakthrough in the search for drugs to treat HFrEF.
Karina Huynh
Nature reviews. Cardiology, 16(12), 700-700 (2019-10-04)
Hiroki Yoshioka et al.
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
Ryo Shibusawa et al.
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
Kazuno Omori et al.
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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