Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.
IC50&Target
Gap junction.
体外研究
Danegaptide (GAP-134, compound 9f; 0.01 nM-100 μM) dose dependently reduces dye uptake in cultured C6 glioma cells in a manner.
体内研究
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.
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.
分子式
C14H18ClN3O4
分子量
327.76
CAS号
943133-81-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-80°C
2 years
-20°C
1 year
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 50 mg/mL (152.55 mM; Sonication is recommended.)
H2O : 50 mg/mL (152.55 mM; Sonication is recommended.)
* (< 1 mg/ml refers to the product slightly soluble or insoluble)