(2R,3R,4R,5S)-2-羟甲基-3,4,5-三羟基哌啶盐酸盐

用途

1-Deoxynojirimycin hydrochloride (Duvoglustat hydrochloride) 是一种口服有效的 α-葡萄糖苷酶 (α-glucosidase) 抑制剂。1-Deoxynojirimycin hydrochloride 抑制餐后血糖,预防糖尿病。1-Deoxynojirimycin hydrochloride 具有降血糖、减肥和抗病毒的作用。

名称

[ CAS 号 ]:
73285-50-4

[ 中文名 ]:
去氧野艽霉素盐酸盐

[ 英文名 ]:
1-Deoxynojirimycin hydrochloride

[英文别名 ]:

(+)-1-deoxynojirimycin hydrochloride
(+-)-1-Chlor-8,9-dihydro-inden
1H-Indene,1-chloro-3a,7a-dihydro
Duvoglustat hydrochloride
1,5-dideoxy-1,5-imino-D-glucitol hydrochloride

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> PI3K/Akt/mTOR 信号通路 >> PI3K

研究领域 >> 代谢疾病

[体内研究]

1-脱氧野吉霉素盐酸盐(盐酸杜夫格鲁司他)(20-80 mg/kg；静脉注射；每日4周)具有减肥作用[3]。1-脱氧野吉霉素盐酸盐通过激活db/db小鼠骨骼肌胰岛素信号转导PI3K/AKT通路显著提高胰岛素敏感性[3]。动物模型：db/db小鼠[3]剂量：20、40、80mg/kg,静脉注射,每日4周,结果：体重、血糖、血清胰岛素水平显著降低,糖耐量、胰岛素耐量明显改善。

[参考文献]

[1]. Gao K, et al. 1-Deoxynojirimycin: Occurrence, Extraction, Chemistry, Oral Pharmacokinetics, Biological Activities and In Silico Target Fishing. Molecules. 2016 Nov 23;21(11). pii: E1600.

[2]. Chaluntorn Vichasilp,et al. Development of high 1-deoxynojirimycin (DNJ) content mulberry tea and use of response surface methodology to optimize tea-making conditions for highest DNJ extraction. LWT - Food Science and Technology. Volume 45, Issue 2, March 2012, Pages 226-232.

[3]. Liu Q, et al. 1-Deoxynojirimycin Alleviates Insulin Resistance via Activation of Insulin Signaling PI3K/AKT Pathway in Skeletal Muscle of db/db Mice. Molecules. 2015 Dec 4;20(12):21700-14.

物理化学性质

[ 密度 ]:
1.456 g/cm3

[ 沸点 ]:
361.1ºC at 760 mmHg

[ 熔点 ]:
195-196ºC

[ 分子式 ]:
C₆H₁₄ClNO₄

[ 分子量 ]:
199.633

[ 闪点 ]:
197.3ºC

[ 精确质量 ]:
199.061142

[ PSA ]:
92.95000

[ 储存条件 ]:
2-8°C，保存于惰性气体中

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/38

[ 安全声明 (欧洲) ]:
S22-S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

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文献

Chemical genetics reveals a complex functional ground state of neural stem cells.

Nat. Chem. Biol. 3(5) , 268-273, (2007)

The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain canc...

Production of the α-glycosidase inhibitor 1-deoxynojirimycin from Bacillus species.

Food Chem. 138(1) , 516-23, (2013)

1-Deoxynojirimycin (DNJ), a potent α-glycosidase inhibitor, has therapeutic applications in treatments of HIV, Gaucher's disease, and diabetes. DNJ has been extracted from natural sources (mulberry le...

Specificity of Processing α-glucosidase I is guided by the substrate conformation: crystallographic and in silico studies.

J. Biol. Chem. 288(19) , 13563-74, (2013)

The enzyme “GluI” is key to the synthesis of critical glycoproteins in the cell.We have determined the structure of GluI, and modeled binding with its unique sugar substrate.The specificity of this in...

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