Lidorestat

• 常用名: Lidorestat
• 英文名: Lidorestat
• CAS号: 245116-90-9
• 分子量: 376.35200
• 密度: 1.55g/cm3
• 沸点: 591.4ºC at 760 mmHg
• 分子式: C₁₈H₁₁F₃N₂O₂S
• 熔点: 177-178 °C
• 闪点: 311.4ºC

Lidorestat用途

Lidorestat (IDD-676) 是一种有效的,选择性的,口服活性的醛糖还原酶 (aldose reductase) 抑制剂,IC50 为 5 nM。Lidorestat 可用于治疗慢性糖尿病并发症。Lidorestat 还可改善神经传导并减少白内障形成。

Lidorestat名称

• 中文名: 利多司他
• 英文名: 2-[3-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]indol-1-yl]acetic acid

Lidorestat生物活性

• 描述: Lidorestat (IDD-676) 是一种有效的,选择性的,口服活性的醛糖还原酶 (aldose reductase) 抑制剂,IC50 为 5 nM。Lidorestat 可用于治疗慢性糖尿病并发症。Lidorestat 还可改善神经传导并减少白内障形成。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 醛糖还原酶
  研究领域 >> 代谢疾病
• 靶点实验:

  IC50: 5 nM (Rldose reductase)[1]

• 体外研究: 从体外实验来看,Liderestat对重组人醛糖还原酶(/h/-ALR2)的IC50为5μM。对重组人醛糖还原酶(/h/-ALR1),Liderestat的IC50为27000μM,其选择性为/h/-ALR1//h/-ALR2为5400:1[1][2]。
• 体内研究: 利多卡因(25毫克/千克/天；口服；每天两次；持续6周；糖尿病小鼠)治疗可降低表达糖尿病hAR小鼠的果糖和死亡率。利得瑞斯特不影响体重[1]。动物模型：糖尿病低密度脂蛋白(LDL)受体缺乏[Ldlr(-/-)]小鼠[1]剂量：25mg/kg/天给药：口服；每日2次；6周结果：糖尿病hAR表达小鼠果糖减少,死亡率降低。
• 参考文献:

  [1]. Noh HL, et al. Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat. J Pharmacol Exp Ther. 2009 Feb;328(2):496-503.

  [2]. Van Zandt MC, et al. Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. J Med Chem. 2005 May 5;48(9):3141-52.

  [3]. Maccari R, et al. Identification of new non-carboxylic acid containing inhibitors of aldose reductase. Bioorg Med Chem. 2010 Jun 1;18(11):4049-55.

Lidorestat物理化学性质

• 密度: 1.55g/cm3
• 沸点: 591.4ºC at 760 mmHg
• 熔点: 177-178 °C
• 分子式: C₁₈H₁₁F₃N₂O₂S
• 分子量: 376.35200
• 闪点: 311.4ºC
• 精确质量: 376.04900
• PSA: 83.36000
• LogP: 4.34370
• InChIKey: KYHVTMFADJNSGS-UHFFFAOYSA-N
• SMILES: O=C(O)Cn1cc(Cc2nc3c(F)c(F)cc(F)c3s2)c2ccccc21
• 蒸汽压: 7.87E-15mmHg at 25°C
• 折射率: 1.681
• 储存条件: 2-8°C

Lidorestat靶点实验

查看更多实验

实验名称：Percent reduction in elevated plasma triglyceride levels in diabetic rats (streptozot... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL874894

实验名称：Volume of distribution was determined in fasted rats after i.v. doses of 10 mg/kg/day 来源：ChEMBL 靶标：N/A External Id：CHEMBL852444

实验名称：Percent reduction in elevated plasma triglyceride levels in diabetic rats (streptozot... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL874898

实验名称：Percent reduction in elevated plasma triglyceride levels in diabetic rats (streptozot... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL874896

实验名称：Percent reduction in elevated plasma triglyceride levels in diabetic rats (streptozot... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL874895

实验名称：Area under the concentration time curve 0-24 hr was determined in fasted rats after p... 来源：ChEMBL 靶标：N/A External Id：CHEMBL840413

实验名称：Percent reduction in elevated plasma triglyceride levels in diabetic rats (streptozot... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL874899

实验名称：Area under the concentration time curve 0-24 hr was determined in fasted rats after i... 来源：ChEMBL 靶标：N/A External Id：CHEMBL840416

实验名称：Ability to lower elevated glucose levels in diabetic rats (streptozotocin treated) mo... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL837028

实验名称：Ability to lower elevated glucose levels in diabetic rats (streptozotocin treated) mo... 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL837027

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Lidorestat英文别名

• UNII-R3734K0M7L
• Lidorestat
• IDD-676
• 3NA