Danegaptide

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。

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库存: 现货

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2mg

￥1912.00

1530.00

- +
5mg

￥2875.00

2300.00

- +
10mg

￥3687.00

2950.00

- +
50mg

￥9987.00

7990.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajce55854
CAS: 943134-39-2
别名: (2S,4R)-1-(2-氨基乙酰基)-4-苯甲酰胺吡咯烷-2-甲酸,GAP-134; ZP 1609
分子式: C14H17N3O4
分子量: 291.3
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

Danegaptide (GAP-134), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. Gap junction.

Gap junction uncoupling can alter conduction pathways and promote cardiac re-entry mechanisms that potentiate many supraventricular arrhythmias, such as atrial fibrillation (AF) and atrial flutter (AFL). Gap junction modifier Danegaptide (GAP-134), showed consistent efficacy on measures of conduction and AF/AFL inducibility in the canine sterile pericarditis model. Danegaptide (GAP-134) is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy, as already confirmed in phase I clinical trials.

[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