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Danegaptide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Danegaptide图片
CAS NO:943134-39-2
规格:98%
分子量:291.3
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
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。
CAS:943134-39-2
分子式:C14H17N3O4
分子量:291.3
纯度:98%
存储:Store at -20°C

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