N6-(1-甲乙基)赖氨酸 | 5977-09-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: N6-(1-甲乙基)赖氨酸
• 中文别名: HL-赖氨酸（异丙基）-OH；N6-(异丙基)-L-赖氨酸
• 英文名称: (S)-2-Amino-6-(isopropylamino)hexanoic acid
• 英文别名: (2S)-2-amino-6-(propan-2-ylamino)hexanoic acid
• CAS: 5977-09-3
• 化学式: C₉H₂₀N₂O₂
• 分子量: 188.27
• InChiKey: CBAWNLIZBXJSFS-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  13
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  75.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• POTENT AND SELECTIVE INHIBITORS OF NAV1.7
  申请人：AMGEN INC

  公开号：US20160024159A1

  公开（公告）日：2016-01-28

  Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Na V 1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Na V 1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

  本文揭示了一种物质组合物，包括一种孤立的多肽，该多肽是一种外周限制的NaV1.7抑制剂。在一些公开的实施方式中，这种孤立的多肽是NaV1.7的抑制剂。其他实施方式是该物质组合物的共轭实施方式和含有该物质组合物的药物组合物。还揭示了编码一些创新多肽的孤立核酸和表达载体以及含有它们的重组宿主细胞。还揭示了一种治疗或预防疼痛的方法。
• COMPOUNDS FOR THE DIAGNOSIS OF DISEASES ASSOCIATED WITH VCAM EXPRESSION
  申请人：Port Marc

  公开号：US20110200533A1

  公开（公告）日：2011-08-18

  The present invention relates to a compound of the following general formula (I): Signal-Linker-Peptide (I) in which: -Signal represents a signal entity; -Linker, which may or may not be present, represents a chemical bond, and -Peptide represents a peptide comprising a VCAM-targeting peptide, the VCAM-targeting peptide being chosen from the peptides of formula below and the functional equivalents thereof: a) X1-X2-X3-X4-X5-X6-X7-X8-X9 (1) (SEQ ID No. 1) where X1 is absent or chosen from cysteine and methionine; X2 chosen from asparagine and glutamine; X3 chosen from asparagine and glutamine; X4 chosen from serine and threonine; X5 chosen from lysine, arginine, histidine and ornithine; X6 chosen from serine and threonine; X7 chosen from histidine, arginine and lysine; X8 chosen from threonine and serine; X9 is absent or chosen from cysteine and methionine; preferably, the peptide CNNSKSHTC (SEQ ID No. 2) and the peptide NNSKSHT (SEQ ID No. 3); b) X10-X11-X12-X13-X14-X15-X16-X17-X18 (2) (SEQ ID No. 4) with X10 chosen from cysteine and methionine; X11 chosen from methionine and cysteine; X12 chosen from lysine, arginine and alanine; X13 chosen from threonine and serine; X14 chosen from aspartic acid and glutamic acid; X15 chosen from threonine and serine; X16 chosen from arginine, alanine and lysine; X17 chosen from leucine, isoleucine and valine; X18 chosen from cysteine and methionine; preferably, the peptide CMKTDTRLC (SEQ ID No. 5); and the pharmaceutically acceptable salts of these compounds of a) or of b).

  本发明涉及以下一般式(I)的化合物：Signal-Linker-Peptide (I)其中：- Signal代表信号实体；- Linker，可以存在也可以不存在，代表化学键；- Peptide代表包含VCAM靶向肽的肽，所述VCAM靶向肽从以下式的肽中选择，以及其功能等效物：a) X1-X2-X3-X4-X5-X6-X7-X8-X9 (1) (序列号1)，其中X1不存在或从半胱氨酸和蛋氨酸中选择；X2从天冬氨酸和谷氨酸中选择；X3从天冬氨酸和谷氨酸中选择；X4从丝氨酸和苏氨酸中选择；X5从赖氨酸、精氨酸、组氨酸和鸟氨酸中选择；X6从丝氨酸和苏氨酸中选择；X7从组氨酸、精氨酸和赖氨酸中选择；X8从苏氨酸和丝氨酸中选择；X9不存在或从半胱氨酸和蛋氨酸中选择；优选的肽为CNNSKSHTC (序列号2)和NNSKSHT (序列号3)；b) X10-X11-X12-X13-X14-X15-X16-X17-X18 (2) (序列号4)，其中X10从半胱氨酸和蛋氨酸中选择；X11从蛋氨酸和半胱氨酸中选择；X12从赖氨酸、精氨酸和丙氨酸中选择；X13从苏氨酸和丝氨酸中选择；X14从天冬氨酸和谷氨酸中选择；X15从苏氨酸和丝氨酸中选择；X16从精氨酸、丙氨酸和赖氨酸中选择；X17从亮氨酸、异亮氨酸和缬氨酸中选择；X18从半胱氨酸和蛋氨酸中选择；优选的肽为CMKTDTRLC (序列号5)；以及a)或b)中的这些化合物的药用盐。
• CYCLIC PEPTIDE CXCR4 ANTAGONISTS
  申请人：Kohn Wayne David

  公开号：US20080300177A1

  公开（公告）日：2008-12-04

  Provided are lactam-cyclized peptide CXCR4 antagonists useful in the treatment of cancers, rheumatoid arthritis, pulmonary fibrosis, and HIV infection.

  提供了在治疗癌症、类风湿关节炎、肺纤维化和HIV感染中有用的内酰胺环化肽CXCR4拮抗剂。
• DIMERIC IAP INHIBITORS
  申请人：STRAUB Christopher Sean

  公开号：US20110206690A1

  公开（公告）日：2011-08-25

  The present invention provides compounds of formula M-L-M′ (where M and M′ are each independently a monomeric moiety of Formula (I) and L is a linker). The dimeric compounds have been found to be effective in promoting apoptosis in rapidly dividing cells.

  本发明提供了公式M-L-M′的化合物（其中M和M′分别是公式（I）中的单体基团，L是连接物）。已发现二聚化合物在促进快速分裂细胞凋亡方面具有有效性。
• COMPOUNDS FOR THE DIAGNOSIS OF APOPTOSIS
  申请人：Port Marc

  公开号：US20100143250A1

  公开（公告）日：2010-06-10

  The present invention relates to a compound of general formula (I) below: Signal−Linker−Peptide (I) in which Signal represents a signal entity; Linker, which may or may not be present, represents a chemical bond and Peptide represents a peptide comprising an apoptosis-targeting peptide, the apoptosis-targeting peptide being chosen from the peptides having the formula below and the functional equivalents thereof: X1-X2-X3-X4-X5-X6 (1) (SEQ ID No 1) in which X1 and X2 represent, independently of one another, leucine or isoleucine, X3 and X4 represent lysine, X5 represents proline and X6 represents phenylalanine, advantageously the peptide L-I-K-K-P-F (SEQ ID No 11) and the functional equivalents thereof; D-A-H-S-X7-S (2) (SEQ ID No 2) in which X7 represents phenylalanine or leucine; P-G-D-L-X8-X9 (3) (SEQ ID No 3) in which X8 represents serine or valine and X9 represents threonine or arginine; H-G-X10-L-S-X11 (4) (SEQ ID No 4) in which X10 represents aspartic acid or histidine, and X11 represents threonine or isoleucine; V-L-G-E-R-G (5) (SEQ ID No 5); and the pharmaceutically acceptable salts of these compounds.

  本发明涉及一种通式（I）化合物：Signal−Linker−Peptide（I），其中Signal代表信号实体；Linker代表可能存在或不存在的化学键；Peptide代表包含凋亡靶向肽的肽，所述凋亡靶向肽选择以下具有通式的肽及其功能等效物：X1-X2-X3-X4-X5-X6（1）（SEQ ID No 1），其中X1和X2分别独立地表示亮氨酸或异亮氨酸，X3和X4表示赖氨酸，X5表示脯氨酸，X6表示苯丙氨酸，优选的肽为L-I-K-K-P-F（SEQ ID No 11）及其功能等效物；D-A-H-S-X7-S（2）（SEQ ID No 2），其中X7表示苯丙氨酸或亮氨酸；P-G-D-L-X8-X9（3）（SEQ ID No 3），其中X8表示丝氨酸或缬氨酸，X9表示苏氨酸或精氨酸；H-G-X10-L-S-X11（4）（SEQ ID No 4），其中X10表示天冬氨酸或组氨酸，X11表示苏氨酸或异亮氨酸；V-L-G-E-R-G（5）（SEQ ID No 5）；以及这些化合物的药学上可接受的盐。