Danegaptide (GAP-134) is a potent, selective and orally activegap-junctionmodifier with an antiarrhythmic effect^[1][2].

Gap junction.

Danegaptide (GAP-134, compound 9f; 0.01 nM-100 μM) dose dependently reduces dye uptake in cultured C6 glioma cells in a manner^[1].

Danegaptide (GAP-134, compound 9f) is evaluated for in vivo efficacy in the mouse CaCl₂model after oral administration. For doses of 5-20 mg/kg po, Danegaptide significantly prolongs the time to conduction block in mice after the infusion of CaCl₂^[1].
Danegaptide (GAP-134) is biologically active upon oral administration at an average plasma concentration of 250 nM, and reduces atrial fibrillation in a dog model. Danegaptide has no effect on heart rate, arterial blood pressure or other electrocardiogram (ECG) parameters. Danegaptide is an effective antiarrhythmic compound in the setting of ischaemia/reperfusion-induced arrhythmogenesis in barbiturate-anesthetized, open-chest beagles^[2].

291.30

C₁₄H₁₇N₃O₄

943134-39-2

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