推薦產品
產品名稱
达格列净, ≥98% (HPLC)
品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D (+7.0° to +13.0°, c = 0.2 in methanol)
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
−20°C
SMILES 字串
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 密鑰
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。
訊號詞
Danger
危險分類
Acute Tox. 4 Oral - Aquatic Chronic 2 - Eye Irrit. 2 - STOT RE 1
標靶器官
Kidney
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
從最近期的版本中選擇一個：
分析證明 (COA)
Lot/Batch Number
Dapagliflozin - a breakthrough in the search for drugs to treat HFrEF.
Karina Huynh
Nature reviews. Cardiology, 16(12), 700-700 (2019-10-04)
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
M Obermeier et al.
Drug metabolism and disposition: the biological fate of chemicals, 38(3), 405-414 (2009-12-10)
(2S,3R,4R,5S,6R)-2-(3-(4-Ethoxybenzyl)-4-chlorophenyl)-6-hydroxymethyl-tetrahydro-2H-pyran-3,4,5-triol (dapagliflozin; BMS-512148) is a potent sodium-glucose cotransporter type II inhibitor in animals and humans and is currently under development for the treatment of type 2 diabetes. The preclinical characterization of dapagliflozin, to allow compound selection and prediction of pharmacological
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
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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