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格列派特

格列派特用途

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。

格列派特名称

[ CAS 号 ]:
25046-79-1

[ 中文名 ]:
格列派特

[ 英文名 ]:
Glisoxepid

[英文别名 ]:

格列派特生物活性

[ 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.

格列派特物理化学性质

[ 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

格列派特毒性和生态

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

格列派特合成路线

详细合成路线

格列派特上下游产品

格列派特上游产品

格列派特下游产品

推荐生产厂家/供应商：

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Glisoxepide

公司名：上海阿拉丁生化科技股份有限公司

区域：上海市浦东新区

价格：
￥2438.0/10mg ￥需询单/1g ￥需询单/1g ￥需询单/1g

联系人：阿拉丁李高志

产品详情：Glisoxepid

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