943133-81-1

• 常用中文名：GAP-134 Hydrochloride
• 常用英文名：GAP-134 (Hydrochloride)
• CAS号：943133-81-1
• 分子式：C₁₄H₁₈ClN₃O₄
• 分子量：327.76300
• 相关类别： 多肽产品
• 发布时间：2017-12-16 22:39:49
• 更新时间：2024-01-07 17:15:31
• GAP-134(Danegaptide, ZP 1609)盐酸盐为修饰的二肽，是第二代口服生物相容性的缝隙连接调节剂。

名称

• 中文名: Danegaptide Hydrochloride
• 英文名: (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid,hydrochloride
• 英文别名: GAP134 Hydrochloride; ZP1609 Hydrochloride; CS-1101; GAP-134 (Hydrochloride)

物化性质

• 分子式: C₁₄H₁₈ClN₃O₄
• 分子量: 327.76300
• 精确质量: 327.09900
• PSA: 116.22000
• LogP: 1.44420
• 储存条件: -20°C

生物活性

• 描述: Danegaptide Hydrochloride (GAP-134 Hydrochloride) 是一种选择性的缝隙连接 (gap junction) 调节剂。
• 相关类别:
  信号通路 >> 细胞骨架 >> 间隙连接蛋白
  多肽产品
  研究领域 >> 心血管疾病
• 靶点:

  Gap junction.

• 参考文献:

  [1]. De Vuyst E, Boengler K, Antoons G, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83.

  [2]. Laurent G, Leong-Poi H, Mangat I, et al. Effects of chronic gap junction conduction-enhancing antiarrhythmic peptide GAP-134 administration on experimental atrial fibrillation in dogs. Circ Arrhythm Electrophysiol. 2009 Apr;2(2):171-8.

  [3]. Hennan JK, Swillo RE, Morgan GA, et al. GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14.

  [4]. Rossman EI, Liu K, Morgan GA, et al. The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33.

  [5]. Eugene L. Piatnitski Cheklera, John A. Buterab, Li Dib, Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters. 2009,19(16): 4551-4554