25046-79-1

• 常用中文名：格列派特
• 常用英文名：Glisoxepid
• CAS号：25046-79-1
• 分子式：C₂₀H₂₇N₅O₅S
• 分子量：449.52400
• 相关类别： 信号通路 跨膜转运 钾通道
• 发布时间：2018-07-05 12:28:31
• 更新时间：2024-01-10 01:07:18
• Glisoxepide 是一种磺胺衍生物,是一种可口服的,非选择性的 K(ATP) 通道阻滞剂,具有抗高血糖活性和心血管调节作用。

名称

• 中文名: 格列派特
• 英文名: N-[2-[4-(azepan-1-ylcarbamoylsulfamoyl)phenyl]ethyl]-5-methyl-1,2-oxazole-3-carboxamide
• 英文别名: Glisoxepida [INN-Spanish]; Glisepin; Glisoxepida; Glisoxepid; Glisoxepide; 5-methyl-isoxazole-3-carboxylic acid 4-(azepan-1-ylcarbamoyl-sulfamoyl)-phenethylamide; Glisoxepida [Spanish]; N-{2-[4-({[(azepan-1-ylamino)carbonyl]amino}sulfonyl)phenyl]ethyl}-5-methylisoxazole-3-carboxamide; Glisoxepidum; Glisoxepidum [INN-Latin]; N-{2-[4-({[(azepan-1-yIamino)carbonyI]amino}suIfonyl)phenyI]ethyI}-5-methylisoxazole-3-carboxamide; Glisoxepide (INN); Pro-Diaban

物化性质

• 密度: 1.37g/cm3
• 分子式: C₂₀H₂₇N₅O₅S
• 分子量: 449.52400
• 精确质量: 449.17300
• PSA: 142.02000
• LogP: 3.92580
• 折射率: 1.617

生物活性

• 描述: Glisoxepide 是一种磺胺衍生物,是一种可口服的,非选择性的 K(ATP) 通道阻滞剂,具有抗高血糖活性和心血管调节作用。
• 相关类别:
  研究领域 >> 心血管疾病
  研究领域 >> 代谢疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点:

  K(ATP) channel[1]

• 体外研究: glishoxepide抑制大鼠肝细胞摄取胆汁酸[3]。glishoxepide以200μM的Ki非竞争性地抑制胆酸的摄取[3]。
• 参考文献:

  [1]. Sato T, et al. Bepridil, an antiarrhythmic drug, opens mitochondrial KATP channels, blocks sarcolemmal KATP channels, and confers cardioprotection. J Pharmacol Exp Ther. 2006 Jan;316(1):182-8. Epub 2005 Sep 20.

  [2]. Selvaag E. Photohemolytic potency of oral antidiabetic drugs in vitro: effects of antioxidants and a nitrogen atmosphere. Photodermatol Photoimmunol Photomed. 1996 Aug;12(4):166-70.

  [3]. Fückel D, et al. Interaction of sulfonylureas with the transport of bile acids into hepatocytes. Eur J Pharmacol. 1992 Mar 31;213(3):393-404.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NY2350000 CHEMICAL NAME : 3-Isoxazolecarboxamide, N-(2-(4-(((((hexahydro-1H-azepin-1-yl)amino)carbonyl) amino)sulfonyl) phenyl)ethyl)-5-methyl- CAS REGISTRY NUMBER : 25046-79-1 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C20-H27-N5-O5-S MOLECULAR WEIGHT : 449.58 WISWESSER LINE NOTATION : T7NTJ AMVMSWR D2MV- ET5NOJ C1 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 196 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 283 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - cyanosis Lungs, Thorax, or Respiration - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >2 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - cat DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : >4 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 24,409,1974

合成路线

39499-34-8 ~% 25046-79-1

文献：Arzneimittel-Forschung, , vol. 24, # 0 p. 363 - 374

6325-22-0 ~% 25046-79-1

文献：Arzneimittel-Forschung, , vol. 24, # 0 p. 363 - 374

24477-36-9 ~% 25046-79-1

文献：Arzneimittel-Forschung, , vol. 24, # 0 p. 363 - 374

5906-35-4 24489-02-9 ~% 25046-79-1

文献：Arzneimittel-Forschung, , vol. 24, # 0 p. 363 - 374

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