| Identification | Back Directory | [Name]
ZP 1609 Hydrochloride | [CAS]
943133-81-1 | [Synonyms]
GAP134 Hydrochloride
ZP1609 Hydrochloride
ZP-1609 Hydrochloride
ZP 1609 Hydrochloride
GAP 134 Hydrochloride
GAP-134 (Hydrochloride)
Danegaptide Hydrochloride
GAP-134 HYDROCHLORIDE, >98%
Danegaptide hydrochloride salt
Danegaptide (GAP-134) hydrochloride
2H5]-Danegaptide hydrochloride salt
GAP-134 hydrochloride
(Danegaptide Hydrochloride
(4R)-Glycyl-4-(benzoylamino)-L-proline hydrochloride (1:1)
4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid
GAP-134 Hydrochloride,Danegaptide Hydrochloride,ZP 1609 Hydrochloride, >98%
(2S;4R)-1-(2-AMINOACETYL)-4-BENZAMIDOPYRROLIDINE-2-CARBOXYLIC ACID;HYDROCHLORIDE
DANEGAPTIDE HYDROCHLORIDE;ZP1609 HYDROCHLORIDE;GAP134 HYDROCHLORIDE;GAP 134 HYDROCHLORIDE;ZP-1609 HYDROCHLORIDE;ZP 1609 HYDROCHLORIDE | [Molecular Formula]
C14H18ClN3O4 | [MDL Number]
MFCD23160032 | [MOL File]
943133-81-1.mol | [Molecular Weight]
327.763 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:55.0(Max Conc. mg/mL);167.81(Max Conc. mM)
H2O:75.0(Max Conc. mg/mL);228.83(Max Conc. mM) | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GAP-134 Hcl (Danegaptide, ZP 1609), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability.
IC50 value:
Target: gap junction
Gap junction uncoupling can alter conduction pathways and promote cardiac re-entry mechanisms that potentiate many supraventricular arrhythmias, such as atrial fibrillation (AF) and atrial flutter (AFL). Gap junction modifier GAP-134, showed consistent efficacy on measures of conduction and AF/AFL inducibility in the canine sterile pericarditis model. GAP-134 is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy, as already confirmed in phase I clinical trials. | [Uses]
Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a potent, selective and orally active gap-junction modifier with an antiarrhythmic effect[1][2]. | [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].
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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]. | [References]
References:[1]. De Vuyst E, Boengler K, Antoons G, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83.
[2]. Laurent G, Leong-Poi H, Mangat I, et al. Effects of chronic gap junction conduction-enhancing antiarrhythmic peptide GAP-134 administration on experimental atrial fibrillation in dogs. Circ Arrhythm Electrophysiol. 2009 Apr;2(2):171-8.
[3]. Hennan JK, Swillo RE, Morgan GA, et al. GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14.
[4]. Rossman EI, Liu K, Morgan GA, et al. The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33.
[5]. Eugene L. Piatnitski Cheklera, John A. Buterab, Li Dib, Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters. 2009,19(16): 4551-4554 |
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