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| | ZP 1609 Hydrochloride Basic information |
| Product Name: | ZP 1609 Hydrochloride | | Synonyms: | Danegaptide Hydrochloride;GAP 134 Hydrochloride;GAP-134 (Hydrochloride);GAP134 Hydrochloride;ZP 1609 Hydrochloride;ZP1609 Hydrochloride;ZP-1609 Hydrochloride;(4R)-Glycyl-4-(benzoylamino)-L-proline hydrochloride (1:1) | | CAS: | 943133-81-1 | | MF: | C14H18ClN3O4 | | MW: | 327.76342 | | EINECS: | | | Product Categories: | | | Mol File: | 943133-81-1.mol |  |
| | ZP 1609 Hydrochloride Chemical Properties |
| 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 |
| | ZP 1609 Hydrochloride Usage And Synthesis |
| 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. | | 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 |
| | ZP 1609 Hydrochloride Preparation Products And Raw materials |
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