GAP-134

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Danegaptide (GAP-134) 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。

A potent, orally active gap-junction modifier; prevents significantly conduction velocity slowing at 10 nM compared with vehicle; has highly desirable in vitro and in vivo safety profile including (1) lack of direct effects on membrane ion currents, hERG inhibition, and CYP450 liabilities, (2) negative AMES result, (3) a benign NovaScreen profile, and (4) no effects on systemic hemodynamics.Heart Arrhythmia Phase 2 Discontinued.

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

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.

Danegaptide | ZP1609 | GAP134 | GAP 134 | ZP-1609 | ZP 1609

Cytoskeleton/Cell Adhesion Molecules

Gap Junction Protein

Gap Junction Protein

Cardiovascular Disease

Heart Arrhythmia

943134-39-2

291.3025

C14H17N3O4

>98% (HPLC)

10 mM in DMSO

C1C(CN(C1C(=O)O)C(=O)CN)NC(=O)C2=CC=CC=C2

L-Proline, glycyl-4-(benzoylamino)-, (4R)-

(-20℃)

With Ice Pack

≥ 2 years