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Danegaptide Sale

(Synonyms: (2S,4R)-1-(2-氨基乙酰基)-4-苯甲酰胺吡咯烷-2-甲酸,GAP-134; ZP 1609) 目录号 : GC35806

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 Chemical Structure

Cas No.:943134-39-2

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2mg
¥1,589.00
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5mg
¥2,385.00
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10mg
¥3,089.00
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50mg
¥8,337.00
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Sample solution is provided at 25 µL, 10mM.

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Description

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

化学性质

Cas No. 943134-39-2 SDF
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
Canonical SMILES O=C(N[C@H]1CN(C(CN)=O)[C@H](C(O)=O)C1)C2=CC=CC=C2
分子式 C14H17N3O4 分子量 291.3
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.4329 mL 17.1644 mL 34.3289 mL
5 mM 0.6866 mL 3.4329 mL 6.8658 mL
10 mM 0.3433 mL 1.7164 mL 3.4329 mL
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