(2S)-3-[2-[(3R)-4-amino-4-oxo-3-(trimethylazaniumyl)butyl]-1H-imidazol-5-yl]-2-azaniumylpropanoate

• 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
• 英文名称: (2S)-3-[2-[(3R)-4-amino-4-oxo-3-(trimethylazaniumyl)butyl]-1H-imidazol-5-yl]-2-azaniumylpropanoate
• 化学式: C13H24N5O3+
• 分子量: 298.36
• InChiKey: FOOBQHKMWYGHCE-VHSXEESVSA-O

计算性质

• 辛醇/水分配系数(LogP)：
  -3.5
• 重原子数：
  21
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  135
• 氢给体数：
  4
• 氢受体数：
  5

文献信息

• [EN] PANTETHENOYLCYSTEINE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS DE PANTÉTHÉNOYLCYSTÉINE ET LEURS UTILISATIONS
  申请人：COMET THERAPEUTICS INC

  公开号：WO2020198573A1

  公开（公告）日：2020-10-01

  The present disclosure relates to compounds of Formula (I) or (II): (Formulae (I), (II)), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

  本公开涉及式(I)或(II)的化合物：(式(I)，(II))，以及其药用可接受的盐或溶剂化合物。本公开还涉及包含这些化合物的药物组合物，以及这些化合物和药物组合物的治疗和诊断用途。
• [EN] MACROCYCLIC PANTETHEINE DERIVATIVES AND USES THEREOF<br/>[FR] DÉRIVÉS MACROCYCLIQUES DE LA PANTÉTHÉINE ET LEURS UTILISATIONS
  申请人：COMET THERAPEUTICS INC

  公开号：WO2021108579A1

  公开（公告）日：2021-06-03

  The present disclosure relates to compounds of Formulae (I) or (II): and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.

  本公开涉及式(I)或(II)的化合物，以及其药学上可接受的盐或溶剂化合物。本公开还涉及包含这些化合物的药物组合物，以及这些化合物和药物组合物的治疗和诊断用途。
• Peptide Tyrosinase Activators
  申请人：Escape Therapeutics, Inc.

  公开号：US20150152139A1

  公开（公告）日：2015-06-04

  Peptides that increase melanin synthesis are provided. These peptides include pentapeptides YSSWY, YRSRK, and their variants. The peptides may activate the enzymatic activity of tyrosinase to increase melanin synthesis. The pharmaceutical, cosmetic, and other compositions including the peptides are also provided. The methods of increasing melanin production in epidermis of a subject are provided where the methods include administering compositions comprising an amount of one or more peptides effective to increase the melanin production. The methods also include treating vitiligo or other hypopigmentation disorders with compositions including one or more peptides.

  提供了增加黑色素合成的肽类。这些肽包括五肽YSSWY、YRSRK及其变体。这些肽可能激活酪氨酸酶的酶活性，以增加黑色素的合成。还提供了包括这些肽的制药、化妆品和其他组合物。提供了一种增加受试者表皮黑色素产生的方法，其中方法包括给予含有一种或多种肽的组合物的有效量以增加黑色素的产生。这些方法还包括使用包括一种或多种肽的组合物治疗白癜风或其他低色素症。
• Imaging of protease activity in live cells using activity based probes
  申请人：Bogyo S. Matthew

  公开号：US20070036725A1

  公开（公告）日：2007-02-15

  Methods and materials for the imaging of cells containing active proteases such as cathepsin are disclosed. The present materials include activity based probes that bind to an enzyme and are subsequently cleaved. Cleavage results in a fluorescent signal due to removal of a quenching group which, when present on the probe causes altered or no fluorescence. The probes employ an acyloxymethyl ketone reactive group, one or more amino acids for determining specificity, a fluorophore and a quencher. The probes are cell permeable and may use, for example, a QSY7 (diarylyrhodamine) quencher and a BODIPY (bora-diaza-indecene) dye.

  揭示了用于成像含有活性蛋白酶（如半胱氨酸蛋白酶）的细胞的方法和材料。目前的材料包括结合到酶并随后被切割的活性基团探针。切割导致荧光信号的产生，因为去除了一个熄灭基团，当存在于探针上时，会导致改变或无荧光。这些探针使用酰氧甲基酮反应基团，一个或多个氨基酸用于确定特异性，一个荧光团和一个熄灭剂。这些探针具有细胞穿透性，例如，可以使用QSY7（二芳基罗丹明）熄灭剂和BODIPY（硼二氮杂环庚烯）染料。
• THERAPEUTIC COMPOUNDS
  申请人：Lavoie Edmond J.

  公开号：US20090156627A1

  公开（公告）日：2009-06-18

  The invention provides compounds of formula I: wherein A, B, D, E, R 1 , R 2 , R 3 , R 4 , R 5 , X, and ----- have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.

  该发明提供了公式I的化合物：其中A、B、D、E、R1、R2、R3、R4、R5、X和-----具有本文中定义的任何值，以及其盐。这些化合物具有作为G-四链体DNA稳定剂和抗增殖剂的活性。