Triacsin c | 76896-80-5

• 物质功能分类: 生物 - 细胞培养 - 添加剂
• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: Triacsin c
• 英文别名: N-[(E)-[(2E,4E,7E)-undeca-2,4,7-trienylidene]amino]nitrous amide
• CAS: 76896-80-5
• 化学式: C₁₁H₁₇N₃O
• 分子量: 207.27
• InChiKey: NKTGCVUIESDXPU-YLEPRARLSA-N

物化性质

• 沸点：
  320.7±45.0 °C(Predicted)
• 密度：
  0.94±0.1 g/cm3(Predicted)
• 溶解度：
  可溶于甲醇：4.90-5.10mg/mL，澄清（淡黄色至黄色）

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  53.8
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• WGK Germany：
  3
• 海关编码：
  29299090

制备方法与用途

生物活性

Triacsin C（WS 1228A）来自金黄色链霉菌（Streptomyces aureofaciens），是一种天然细胞内长链酰基辅酶A合成酶（ACSL）抑制剂。它通过抑制ACSL来阻止三酰甘油（TAG）积累成脂滴（LD）。Triacsin C对轮状病毒复制具有显著效果。

靶点

• ACSL

反应信息

• 作为产物：
  描述：

  (E,E,E)-2,4,7-undecatrienal 生成 Triacsin c
  参考文献：
  名称：

  YOSHIDA, KEIZO;TANAKA, HIROKAZU;OKAMOTO, MASANORI;IGUCHI, EIKO;KOHSAKA, M+

  摘要：

  DOI：

文献信息

• Combination therapy involving a sodium-hydrogen exchanger type 1 or NHE-1 inhibitor for use in treatment of ischemia
  申请人：Pfizer Products Inc.

  公开号：EP1226830A2

  公开（公告）日：2002-07-31

  The invention provdes methods of reducing tissue damage resulting from ischemia which comprise administering to a mammal in need of such reduction an effective amount of a combination, or a pharmaceutical composition comprising such combination, of an NHE-1 inhibitor and a second compound selected from the group consisting of: (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator. The invention further provides pharmaceutical compositions comprising an amount of an NHE-1 inhibitor; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor; and, preferably, a pharmaceutically acceptable pharmaceutically acceptable carrier, vehicle, or diluent. The invention further provides kits comprising an amount of a sodium-hydrogen exchanger type-1 inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a first unit dosage form; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a thrombin-activatable fibrinolysis inhibitor (TAFI) inhibitor, an activated thrombin-activatable fibrinolysis inhibitor (TAFIa) inhibitor, a Na+/Ca+2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a second unit dosage form; and a container.

  本发明提供了减少缺血导致的组织损伤的方法，该方法包括向需要减少损伤的哺乳动物施用有效量的 NHE-1 抑制剂和选自以下组别的第二种化合物的组合或包含这种组合的药物组合物：(a) 补体调节剂，(b) 代谢调节剂，(c) 抗凋亡剂，(d) 一氧化氮合酶相关剂，和 (e) 酶/蛋白调节剂。本发明进一步提供了药物组合物，其中包含一定量的 NHE-1 抑制剂；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗凋亡剂；(d) 一氧化氮合酶相关剂；以及选自以下组别的酶/蛋白调节剂：蛋白激酶 C 激活剂、内皮素转换酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和多（ADP 核糖）合成酶（PARS/PARP）抑制剂；以及，优选药学上可接受的载体、载体或稀释剂。本发明进一步提供了包含一定量的钠-氢交换剂型-1 抑制剂和药学上可接受的载体、载体或稀释剂的试剂盒，试剂盒为第一单位剂型；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗细胞凋亡剂；(d) 一氧化氮合酶相关剂；(e) 酶/蛋白调节剂，选自以下组别：蛋白激酶 C 激活剂；内皮素转换酶抑制剂；凝血酶激活的可凝血酶抑制剂、凝血酶活化性纤维蛋白溶解抑制剂（TAFI）抑制剂、活化的凝血酶活化性纤维蛋白溶解抑制剂（TAFIa）抑制剂、Na+/Ca+2 交换异构体-1（NCX-1）抑制剂和聚（ADP 核糖）合成酶（PARS/PARP）抑制剂，以及药学上可接受的载体、载体或稀释剂组成的组；以及一个容器。
• PROPHYLACTIC/THERAPEUTIC AGENT FOR CANCER
  申请人：JAPANESE FOUNDATION FOR CANCER RESEARCH

  公开号：EP2018873A1

  公开（公告）日：2009-01-28

  The present invention provides a preventative/therapeutic agent for cancer capable of selectively and effectively killing cancer cells. A medicament of the present invention prepared by combining at least one selected from a substance that inhibits the activity of an enzyme belonging to the acyl-CoA synthase family and a substance that inhibits expression of a gene for an enzyme belonging to the acyl-CoA synthase family, with at least one selected from a substance that inhibits the activity of fatty acid synthase and a substance that inhibits expression of a fatty acid synthase gene and the like can be used as a preventative/therapeutic agent for cancer capable of selectively and effectively killing cancer cells.

  本发明提供了一种能够选择性地有效杀死癌细胞的癌症预防/治疗剂。本发明的药物由至少一种选自抑制酰基-CoA 合酶家族酶活性的物质和抑制酰基-CoA 合酶家族酶基因表达的物质，以及至少一种选自抑制脂肪酸合酶活性的物质和抑制脂肪酸合酶基因表达的物质等制备而成，可用作癌症预防/治疗剂，能够选择性地有效杀死癌细胞。
• METHODS OF TREATING LIVER DISEASE
  申请人：The J. David Gladstone Institutes

  公开号：EP3025727A1

  公开（公告）日：2016-06-01

  The present invention provides methods of treating liver steatosis, liver fibrosis and hepatitis C virus (HCV) infection; methods described include methods of reducing the incidence of complications associated with HCV and cirrhosis of the liver; and methods of reducing viral load, or reducing the time to viral clearance, or reducing morbidity or mortality in the clinical outcomes, in patients suffering from HCV infection.

  本发明提供了治疗肝脏脂肪变性、肝纤维化和丙型肝炎病毒（HCV）感染的方法；所述方法包括降低HCV和肝硬化相关并发症发病率的方法；以及降低HCV感染患者病毒载量、或缩短病毒清除时间、或降低临床结果中发病率或死亡率的方法。
• COMBINATION THERAPY
  申请人：——

  公开号：US20020099075A1

  公开（公告）日：2002-07-25

  The invention provdes methods of reducing tissue damage resulting from ischemia which comprise administering to a mammal in need of such reduction an effective amount of a combination, or a pharmaceutical composition comprising such combination, of an NHE-1 inhibitor and a second compound selected from the group consisting of: (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator. The invention further provides pharmaceutical compositions comprising an amount of an NHE-1 inhibitor; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a tissue-activated fibrinolytic inhibitor (TAFI), a Na + /Ca +2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor; and, preferably, a pharmaceutically acceptable pharmaceutically acceptable carrier, vehicle, or diluent. The invention further provides kits comprising an amount of a sodium-hydrogen exchanger type-1 inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a first unit dosage form; an amount of a second compound selected from the group consisting of (a) a complement modulator, (b) a metabolic modulator, (c) an anti-apoptotic agent, (d) a nitric oxide synthase-related agent, and (e) an enzyme/protein modulator selected from the group consisting of a protein kinase C activator, an endothelin converting enzyme inhibitor, a tissue-activated fibrinolytic inhibitor (TAFI), a Na + /Ca +2 exchanger isoform-1 (NCX-1) inhibitor, and a poly (ADP ribose) synthetase (PARS/PARP) inhibitor, and a pharmaceutically acceptable carrier, vehicle, or diluent in a second unit dosage form; and a container.

  本发明提供了减少缺血导致的组织损伤的方法，该方法包括向需要减少损伤的哺乳动物施用有效量的NHE-1抑制剂和选自以下组的第二种化合物的组合或包含这种组合的药物组合物：(a)补体调节剂，(b)代谢调节剂，(c)抗细胞凋亡剂，(d)一氧化氮合酶相关剂，和(e)酶/蛋白调节剂。本发明进一步提供了药物组合物，该药物组合物包含一定量的 NHE-1 抑制剂；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗细胞凋亡剂；(d) 一氧化氮合酶相关剂；以及选自以下组别的酶/蛋白质调节剂：蛋白激酶 C 激活剂、内皮素转换酶抑制剂、组织活化纤溶抑制剂 (TAFI)、Na. 加 /Ca 2 交换剂同工酶-1（NCX-1）抑制剂和聚（ADP 核糖）合成酶（PARS/PARP）抑制剂；以及，优选药学上可接受的载体、载体或稀释剂。本发明进一步提供了包含一定量的钠-氢交换机 1 型抑制剂和药学上可接受的载体、载体或稀释剂的试剂盒，试剂盒为第一单位剂型；一定量的选自以下组别的第二种化合物：(a) 补体调节剂；(b) 代谢调节剂；(c) 抗凋亡剂；(d) 一氧化氮合酶相关剂；(e) 酶/蛋白调节剂，选自以下组别：蛋白激酶 C 激活剂、内皮素转换酶抑制剂、组织活化纤溶抑制剂（TAFI）、Na 加 /Ca 2 交换剂同工酶-1（NCX-1）抑制剂和聚（ADP 核糖）合成酶（PARS/PARP）抑制剂，以及药学上可接受的载体、载体或稀释剂的第二单位剂型；和容器。
• YOSHIDA, KEIZO;TANAKA, HIROKAZU;OKAMOTO, MASANORI;IGUCHI, EIKO;KOHSAKA, M+
  作者：YOSHIDA, KEIZO、TANAKA, HIROKAZU、OKAMOTO, MASANORI、IGUCHI, EIKO、KOHSAKA, M+

  DOI：——

  日期：——