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Merck
CN

SML2758

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:
960404-48-2
分子量:
502.98
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD28167768

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产品名称

达格列净丙二醇一水合物, ≥98% (HPLC)

SMILES string

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

assay

≥98% (HPLC)

form

powder

optical activity

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

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

Quality Level

100

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相关类别

Biochem/physiol Actions

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000464338
0000464338
0000448523
0000448524
0000448524

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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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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
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