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Merck
CN

SML2758

Sigma-Aldrich

达格列净丙二醇一水合物

≥98% (HPLC), SGLT2 inhibitor, powder

别名:

(1S)-1,5-酐-1-C-[4-氯-3-[(4-乙氧基苯基)甲基]苯基]-D-葡萄糖醇(S)-丙烷-1,2-二醇(1:1)一水合物, BMS 512148 丙二醇水合物, BMS-512148 丙二醇水合物, 达格列净丙二醇水合物, 达格列净(S)-丙二醇一水合物, (2S,3R,4R,5S,6R)-2-(3-(4-乙氧基苄基)-4-氯苯基)-6-羟甲基-四氢-2H-吡喃-3,4,5-三醇丙二醇一水合物

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关于此项目

经验公式(希尔记法):
C21H25ClO6·C3H8O2·H2O
化学文摘社编号:
分子量:
502.98
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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产品名称

达格列净丙二醇一水合物, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

powder

旋光性

[α]/D +17 to +25, c = 1.0 in chloroform-d

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

SMILES字符串

Clc1c(cc(cc1)[C@@H]3O[C@@H]([C@H]([C@@H]([C@H]3O)O)O)CO)Cc2ccc(cc2)OCC.O[C@H](CO)C.O

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 key

GOADIQFWSVMMRJ-UPGAGZFNSA-N

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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

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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分析证书(COA)

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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
Fengjuan Huang et al.
Frontiers in endocrinology, 10, 441-441 (2019-07-25)
Tubulointerstitial fibrosis (TIF) plays an important role in the progression of renal fibrosis in diabetic nephropathy (DN). Accumulating evidence supports a crucial inhibitory effect of dapagliflozin, a SGLT2 inhibitor, on TIF, but the underlying mechanisms remain largely unknown. This study
Nannan Zhang et al.
Cardiovascular diabetology, 18(1), 107-107 (2019-08-21)
Heart failure with preserved ejection fraction (HFpEF) is a difficult disease with high morbidity and mortality rates and lacks an effective treatment. Here, we report the therapeutic effect of dapagliflozin, a sodium-glucose cotransporter 2 inhibitor (SGLT2i), on hypertension + hyperlipidemia-induced HFpEF in a
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

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