Danegaptide

• 常用名: Danegaptide
• 英文名: GAP-134
• CAS号: 943134-39-2
• 分子量: 291.30200
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₄H₁₇N₃O₄
• 熔点: N/A
• 闪点: N/A

Danegaptide用途

Danegaptide (GAP-134) 是修饰的二肽,是第二代口服生物相容性的间隙连接调节剂。

Danegaptide名称

• 中文名: Danegaptide
• 英文名: (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid

Danegaptide生物活性

• 描述: Danegaptide (GAP-134) 是修饰的二肽,是第二代口服生物相容性的间隙连接调节剂。
• 相关类别:
  信号通路 >> 细胞骨架 >> 间隙连接蛋白
  研究领域 >> 心血管疾病
• 靶点实验:

  Gap junction.

• 体外研究: 间隙连接解偶联可改变传导途径并促进心脏再入机制,其加强许多室上性心律失常,例如心房颤动(AF)和心房扑动(AFL)。间隙连接修饰物Danegaptide(GAP-134)在犬无菌性心包炎模型中对传导和AF/AFL诱导能力的测量显示出一致的功效。 Danegaptide(GAP-134)是一种药物制剂,具有良好的临床安全性和潜在的抗心律失常功效,已在I期临床试验中得到证实。
• 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

Danegaptide物理化学性质

• 分子式: C₁₄H₁₇N₃O₄
• 分子量: 291.30200
• 精确质量: 291.12200
• PSA: 116.22000
• LogP: 0.64220
• InChIKey: BIZKIHUJGMSVFD-MNOVXSKESA-N
• SMILES: NCC(=O)N1CC(NC(=O)c2ccccc2)CC1C(=O)O
• 储存条件: 2-8℃

Danegaptide靶点实验

查看更多实验

实验名称：Stability in rat plasma after 3 hrs 来源：ChEMBL 靶标：Plasma External Id：CHEMBL1056450

实验名称：Clearance in dog at 1 mg/kg, iv 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060727

实验名称：Antiarrhythmic activity in calcium chloride-induced mouse arrhythmia model assessed a... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL1056449

实验名称：AUC in dog at 5 mg/kg, po 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060734

实验名称：Antiarrhythmic activity in calcium chloride-induced mouse arrhythmia model assessed a... 来源：ChEMBL 靶标：Mus musculus External Id：CHEMBL1060702

实验名称：Tmax in dog at 5 mg/kg, po 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060733

实验名称：Oral bioavailability in dog at 5 mg/kg 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060730

实验名称：Half life in dog at 5 mg/kg, po 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060731

实验名称：Volume of distribution at steady state in dog at 1 mg/kg, iv 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060728

实验名称：Half life in dog at 1 mg/kg, iv 来源：ChEMBL 靶标：Canis lupus familiaris External Id：CHEMBL1060729

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Danegaptide英文别名

• zp1609
• danegaptide
• gap-134
• unii-pa0y7735at