N-[2-(甲氨基)乙基]-5-异喹啉磺酰胺二盐酸盐 | 84478-11-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异喹啉及其衍生物
• 中文名称: N-[2-(甲氨基)乙基]-5-异喹啉磺酰胺二盐酸盐
• 中文别名: N-[2-(甲氨基)乙基]-5-异喹啉黄酰胺二盐酸盐
• 英文名称: N-(2-methylaminoethyl)-5-isoquinolinesulfonamide
• 英文别名: H-8；N-(2-[methylamino]ethyl)-5-isoquinolinesulfonamide；N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide；H8；N-[2-(methylamino)ethy]-5-isoquinoline sulfonamide；N-(2-(Methylamino)ethyl)-5-isoquinolinesulfonamide；N-[2-(methylamino)ethyl]isoquinoline-5-sulfonamide
• CAS: 84478-11-5
• 化学式: C₁₂H₁₅N₃O₂S
• mdl: MFCD14560562
• 分子量: 265.336
• InChiKey: PJWUXKNZVMEPPH-UHFFFAOYSA-N

物化性质

• 熔点：
  238-246°C dec.
• 溶解度：
  乙醇：25 mg/mL，澄清，无色

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  18
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  79.5
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 危险品标志：
  Xi
• 安全说明：
  S22,S24/25
• 危险类别码：
  R36/37/38
• WGK Germany：
  3

反应信息

• 作为反应物：
  描述：

  S-甲基异硫脲硫酸盐 、 N-[2-(甲氨基)乙基]-5-异喹啉磺酰胺二盐酸盐 在 sodium hydroxide 作用下， 以 水 为溶剂， 反应 3.0h， 以21%的产率得到1-[2-(Isoquinolin-5-ylsulfonylamino)ethyl]-1-methylguanidine;hydrochloride
  参考文献：
  名称：

  5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives

  摘要：

  Two novel series of N-(2-guanidinoalkyl)-5-isoquinolinesulfonamides, 2 and 3, were prepared. Many of the compounds possessed vasodilatory activity when injected locally into the femoral artery of dogs. The most potent compound, 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiazepine, 33, was comparable to diltiazem, which is used clinically as a vasodilator.

  DOI：

  10.1021/jm00121a009
• 作为产物：
  描述：

  异喹啉-5-磺酰氯 在 吡啶 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 3.0h， 生成 N-[2-(甲氨基)乙基]-5-异喹啉磺酰胺二盐酸盐
  参考文献：
  名称：

  5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives

  摘要：

  Two novel series of N-(2-guanidinoalkyl)-5-isoquinolinesulfonamides, 2 and 3, were prepared. Many of the compounds possessed vasodilatory activity when injected locally into the femoral artery of dogs. The most potent compound, 1-amidino-4-(5-isoquinolylsulfonyl)-1,4-perhydrodiazepine, 33, was comparable to diltiazem, which is used clinically as a vasodilator.

  DOI：

  10.1021/jm00121a009

文献信息

• Isoquinolinesulfonyl derivatives and process for the preparation thereof
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04456757A1

  公开（公告）日：1984-06-26

  A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one; R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; or R.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group; R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, and aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  一种Formula (I)的5-异喹啉磺酰衍生物：其中l为零或一；m和n均为1至9的整数；m+n至少为一个整数；R.sub.1为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基或芳基；或R.sub.2和R.sub.3各自为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基，芳基或芳基烷基；R.sub.2和R.sub.3为C.sub.1-6烷基基团，并直接或通过氧原子连接形成与相邻氮原子共轭的5-至7-成员杂环环；或##STR2##基团为##STR3##基团，其中R.sub.4和R.sub.5各自为氢原子，C.sub.1-10烷基，芳基或芳基烷基，R.sub.6为氢原子，C.sub.1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR4##基团，其中R.sub.7为C.sub.1-8烷基；以及其药学上可接受的盐；以及其制备方法。该发明的化合物对血管平滑肌具有松弛作用，并可用作血管扩张剂和降压剂。
• Isoquinolinesulfonyl derivatives
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04525589A1

  公开（公告）日：1985-06-25

  A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; or R.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group; R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## group is a ##STR3## group wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR4## group wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  公式（I）的5-异喹啉磺酰衍生物：##STR1## 其中l为零或一；m和n均为1至9的整数；m+n至少为1的整数；R.sub.1为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基或芳基；或R.sub.2和R.sub.3均为氢原子，C.sub.1-10烷基，C.sub.5-6环烷基，芳基或芳基烷基；R.sub.2和R.sub.3是C.sub.1-6烷基，直接或通过氧原子与相邻的氮原子形成5-至7-成员杂环环；或##STR2##基团是##STR3##基团，其中R.sub.4和R.sub.5均为氢原子，C.sub.1-10烷基，芳基或芳基烷基，R.sub.6为氢原子，C.sub.1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR4##基团，其中R.sub.7为C.sub.1-8烷基；以及其药学上可接受的盐；以及其制备过程。该发明化合物对血管平滑肌具有松弛作用，可用作扩血管剂和降压剂。
• Isoquinolinesulfonyl derivatives which possess a relaxatory action
  申请人：Asahi Kasei Kogyo Kabushiki Kaisha

  公开号：US04560755A1

  公开（公告）日：1985-12-24

  A 5-isoquinolinesulfonyl derivative of Formula (I): ##STR1## wherein l is zero or one; m and n each is an integer of one to nine; m+n is an integer of at least one; R.sub.1 is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group or an aryl group; or R.sub.2 and R.sub.3 each is a hydrogen atom, a C.sub.1-10 alkyl group, a C.sub.5-6 cycloalkyl group, an aryl group or an aralkyl group; R.sub.2 and R.sub.3 are C.sub.1-6 alkylene groups and linked directly or through an oxygen atom to form a 5- to 7-membered heterocyclic ring with the adjacent nitrogen atom; or the ##STR2## wherein R.sub.4 and R.sub.5 each is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group or an aralkyl group and R.sub.6 is a hydrogen atom, a C.sub.1-10 alkyl group, an aryl group, an aralkyl group, a benzoyl group, a cinnamyl group, a cinnamoyl group, a furoyl group or a ##STR3## wherein R.sub.7 is a C.sub.1-8 alkyl group; and the pharmaceutically acceptable salt thereof; and a process for the preparation thereof. The compounds of this invention have a relaxatory action for vascular smooth muscle and are useful as a vasodilator and a hypotensor.

  公式（I）的5-异喹啉磺酰衍生物：##STR1## 其中l为零或一；m和n各为1到9的整数；m+n至少为1的整数；R1为氢原子，C1-10烷基，C5-6环烷基或芳基；或R2和R3各为氢原子，C1-10烷基，C5-6环烷基，芳基或芳基烷基；R2和R3为C1-6烷基，直接或通过氧原子与相邻的氮原子连接，形成5-至7-成员的杂环环与；或##STR2## 其中R4和R5各为氢原子，C1-10烷基，芳基或芳基烷基，R6为氢原子，C1-10烷基，芳基，芳基烷基，苯甲酰基，肉桂基，肉桂酰基，呋喃基或##STR3## 其中R7为C1-8烷基；以及其药学上可接受的盐；以及其制备过程。本发明的化合物具有血管平滑肌松弛作用，可用作血管扩张剂和降压剂。
• METHOD FOR CULTURING HUMAN PLURIPOTENT STEM CELLS
  申请人：National Institute of Biomedical Innovation

  公开号：EP2671945A1

  公开（公告）日：2013-12-11

  An aim of the present invention is to provide a method for culturing a human pluripotent stem cell while maintaining an undifferentiated state, more efficiently than conventional methods, and a kit therefor. The pluripotency of a stem cell was found to be maintained at a high rate, regardless of experimenter's proficiency in culturing techniques, by (a) culturing a human pluripotent stem cell in a first medium which is a medium for pluripotent stem cell comprising activin; (b) replacing the first medium with a second medium which is a medium for pluripotent stem cell comprising no activin, and culturing the human pluripotent stem cell, (c) subculturing the human pluripotent stem cell into the first medium, and then repeating the above (b) and (c) sequentially.

  本发明的目的是提供一种比传统方法更有效的培养人类多能干细胞同时保持未分化状态的方法及其试剂盒。研究发现，无论实验者对培养技术的熟练程度如何，干细胞的多能性都能通过以下方法保持：(a) 在第一培养基中培养人类多能干细胞，该培养基是含有活化素的多能干细胞培养基；(b) 用第二种培养基取代第一种培养基，第二种培养基是不含活化素的多能干细胞培养基，并培养人多能干细胞， (c) 将人多能干细胞亚培养到第一种培养基中，然后依次重复上述(b)和(c)。
• Method and apparatus for measuring protein post-translational modification
  申请人：ICAGEN, INC.

  公开号：US10577642B2

  公开（公告）日：2020-03-03

  The present invention includes a method for analyzing reactions. The method includes the steps of providing a solution of at least one acceptor chemical and at least one donor chemical. The donor chemical is capable of donating a chemical moiety to the acceptor chemical. The solution further includes at least one controller chemical that affects the reaction between the donor chemical and the acceptor chemical. The solution is then incubated so that a portion of the acceptor chemical reacts with the donor chemical to form an acceptor product. Unreacted donor chemical is separated from the acceptor product. The acceptor product or the donor chemical is then measured using X-ray fluorescence. Another aspect of the present invention includes a method for analyzing protein function. The method includes the steps of providing a solution of at least one acceptor chemical and at least one donor chemical. The donor chemical is capable of donating a chemical moiety to the acceptor chemical. The donor chemical includes a functional group selected from ester, anhydride, imide, acyl halide, and amide. The solution is then incubated so that a portion of the acceptor chemical reacts with the donor chemical to form an acceptor product. Unreacted donor chemical is separated from the acceptor product. The acceptor product or the donor chemical is then measured using X-ray fluorescence. Yet another aspect of the present invention includes a method for analyzing protein function. The method includes the steps of providing a solution of at least one acceptor chemical and at least one donor chemical. The solution is then incubated so that a portion of the acceptor chemical reacts with the donor chemical to form an acceptor product. Unreacted donor chemical is separated from the acceptor product. The acceptor product or the donor chemical is then measured using X-ray fluorescence. An additional analytical method is also used to measure either the acceptor product or the donor chemical.

  本发明包括一种分析反应的方法。该方法包括以下步骤：提供至少一种受体化学物质和至少一种供体化学物质的溶液。供体化学物质能够向受体化学物质捐献一个化学分子。溶液还包括至少一种可影响供体化学物质和受体化学物质之间反应的控制化学物质。然后对溶液进行培养，使部分受体化学物质与供体化学物质发生反应，形成受体产物。未反应的供体化学物质与受体产物分离。然后使用 X 射线荧光测量受体产物或供体化学物质。本发明的另一方面包括一种分析蛋白质功能的方法。该方法包括以下步骤：提供至少一种受体化学品和至少一种供体化学品的溶液。供体化学物质能够向受体化学物质提供一个化学分子。供体化学品包括选自酯、酸酐、酰亚胺、酰卤和酰胺的官能团。然后对溶液进行培养，使部分受体化学物质与供体化学物质发生反应，形成受体产物。未反应的供体化学物质与受体产物分离。然后使用 X 射线荧光测量受体产物或供体化学物质。本发明的另一方面包括一种分析蛋白质功能的方法。该方法包括以下步骤：提供至少一种受体化学品和至少一种供体化学品的溶液。然后对溶液进行培养，使部分受体化学物质与供体化学物质发生反应，形成受体产物。未反应的供体化学物质从受体产物中分离出来。然后使用 X 射线荧光测量受体产物或供体化学物质。还可使用另一种分析方法来测量受体产物或供体化学品。