Danegaptide Hydrochloride (GAP-134 Hydrochloride) 是一种有效的，选择性的，具有口服活性的 gap-junction 修饰剂，具有抗心律不齐的作用。

Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect.

Solid

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Danegaptide (GAP-134, compound 9f) is evaluated for in vivo efficacy in the mouse CaCl 2 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 CaCl 2 .
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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisturePowder -80°C 2 years；-20°C 1 year

[1]. John A Butera, et al. Discovery of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride (GAP-134)13, an orally active small molecule gap-junction modifier for the treatment of atrial fibrillation. J Med Chem. 2009 Feb 26;52(4):
[2]. Elke De Vuyst, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83.

In Vitro: DMSO : ≥ 55 mg/mL (167.81 mM)H₂O : ≥ 50 mg/mL (152.55 mM)