Danegaptide

Danegaptide (GAP-134) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect^[1][2]. IC50 & Target: Gap junction. In Vitro: Danegaptide (GAP-134, compound 9f; 0.01 nM-100 μM) dose dependently reduces dye uptake in cultured C6 glioma cells in a manner^[1]. In Vivo: Danegaptide (GAP-134, compound 9f) is evaluated for in vivo efficacy in the mouse CaCl₂ model 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].