28380-24-7

• 常用中文名：尼日尼亚菌素
• 常用英文名：Antibiotic K178
• CAS号：28380-24-7
• 分子式：C₄₀H₆₈O₁₁
• 分子量：746.943
• 相关类别： 信号通路 细胞凋亡 细胞凋亡
• 发布时间：2018-09-10 12:34:17
• 更新时间：2024-01-02 21:38:06
• Nigericin 是一种源自吸水链霉菌的抗生素,可以充当一种离子载体 (K+/H+ ionophore),促进跨线粒体膜的 K+/H+ 交换。Nigericin 可以 NALP3 依赖性方式诱导 IL-1β 释放,可作为 NLRP3 活化剂。Nigericin 触发红细胞衰亡,与 ROS 的形成同时发生,部分是由于氧化应激的诱导。Nigericin 引发细胞凋亡 (apoptosis)。

名称

• 中文名: 尼日利亚菌素
• 英文名: nigericin
• 英文别名: Nigericin; HELIXIN C; 2H-Pyran-2-acetic acid, tetrahydro-6-[[(2S,4R,5R,9R,10R)-9-methoxy-2,4,10-trimethyl-2-[(2S,3'R)-octahydro-2,3'-dimethyl-5'-[(3S,5R,6R)-tetrahydro-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyl-2H-pyran-2-yl][2,2'-bifuran]-5-yl]-1,6-dioxaspiro[4.5]dec-7-yl]methyl]-α,3-dimethyl-, sodium salt, (αS,3R)- (1:1); Sodium (2S)-2-[(3R)-6-{[(2S,4R,5R,9R,10R)-2-{(2S,3'R)-5'-[(3S,5R,6R)-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyltetrahydro-2H-pyran-2-yl]-2,3'-dimethyloctahydro-2,2'-bifuran-5-yl}-9-methoxy-2,4,10-trimethyl-1,6-dioxaspiro[4.5]dec-7-yl]methyl}-3-methyltetrahydro-2H-pyran-2-yl]propanoate; ANTIBIOTIC K178; NIGERICIN NA; AZALOMYCIN M; 2H-Pyran-2-acetic acid, tetrahydro-6-[[(2S,4R,5R,9R,10R)-9-methoxy-2,4,10-trimethyl-2-[(2S,3'R)-octahydro-2,3'-dimethyl-5'-[(3S,5R,6R)-tetrahydro-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyl-2H-pyran-2-yl ;][2,2'-bifuran]-5-yl]-1,6-dioxaspiro[4.5]dec-7-yl]methyl]-α,3-dimethyl-, sodium salt, (αS,3R)- (1:1); POLYETHERIN A; Helix c; x-464

物化性质

• 密度: 1.19g/cm3
• 沸点: 779.9ºC at 760mmHg
• 熔点: 245-255ºC
• 分子式: C₄₀H₆₈O₁₁
• 分子量: 746.943
• 闪点: 226.9ºC
• 精确质量: 746.458130
• PSA: 145.20000
• LogP: 4.37090
• 外观性状: 白色固体
• 折射率: 1.543
• 储存条件: 2-8°C

生物活性

• 描述: Nigericin 是一种源自吸水链霉菌的抗生素,可以充当一种离子载体 (K+/H+ ionophore),促进跨线粒体膜的 K+/H+ 交换。Nigericin 可以 NALP3 依赖性方式诱导 IL-1β 释放,可作为 NLRP3 活化剂。Nigericin 触发红细胞衰亡,与 ROS 的形成同时发生,部分是由于氧化应激的诱导。Nigericin 引发细胞凋亡 (apoptosis)。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
• 靶点:

  K+/H+ ionophore[1]

• 参考文献:

  [1]. Zotova L, et al. Novel components of an active mitochondrial K(+)/H(+) exchange. J Biol Chem. 2010 May 7;285(19):14399-414.

  [2]. Mariathasan S, et al.Cryopyrin activates the inflammasome in response to toxins and ATP.Nature. 2006 Mar 9;440(7081):228-32.

  [3]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : QT6825000 CHEMICAL NAME : Nigericin CAS REGISTRY NUMBER : 28380-24-7 LAST UPDATED : 199612 DATA ITEMS CITED : 2 MOLECULAR FORMULA : C40-H68-O11 MOLECULAR WEIGHT : 725.08 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 190 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : 85GDA2 "CRC Handbook of Antibiotic Compounds," Vols.1- , Berdy, J., Boca Raton, FL, CRC Press, 1980- Volume(issue)/page/year: 5,477,1981 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2500 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 1,594,1951

安全

• 危害码 (欧洲): T: Toxic;
• 危险品运输编码: UN 3462 6
• 包装等级: III
• 危险类别: 6.1(b)

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