ChemicalBook--->CAS DataBase List--->943133-81-1

943133-81-1

943133-81-1 Structure

943133-81-1 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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.
[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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