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ZP 1609 - CAS 943134-39-2

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Category
Inhibitor
Product Name
ZP 1609
Catalog Number
943134-39-2
Synonyms
GAP-134;(2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid;Danegaptide;GAP 134; ZP-1609
CAS Number
943134-39-2
Description
ZP 1609, a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. It is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy, which is confirmed in phase I clinical trials. It is used for the treatment of atrial fibrillation. It improves conduction and reduces atrial fibrillation or flutter in the canine sterile pericarditis model. It prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. It showed consistent efficacy on measures of conduction and AF/AFL inducibility in the canine sterile pericarditis model. It was developed by Zealand Pharma and was termination in Clinical phase II.
Molecular Weight
291.30
Molecular Formula
C14H17N3O4
Quantity
Milligrams-Grams
Quality Standard
In-house standard
COA
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MSDS
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Canonical SMILES
C1C(CN(C1C(=O)O)C(=O)CN)NC(=O)C2=CC=CC=C2
InChI
InChI=1S/C14H17N3O4/c15-7-12(18)17-8-10(6-11(17)14(20)21)16-13(19)9-4-2-1-3-5-9/h1-5,10-11H,6-8,15H2,(H,16,19)(H,20,21)/t10-,11+/m1/s1
InChIKey
BIZKIHUJGMSVFD-MNOVXSKESA-N
Targets
Gap Junction Protein
Current Developer
ZP 1609 was developed by Zealand Pharma and was termination in Clinical phase II.
Structure
CAS 943134-39-2 ZP 1609
Specification
Purity
>98 %
Boiling Point
642.4±55.0 °C | Condition: Press: 760 Torr
Density
1.38±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
Appearance
Solid powder
Application
ZP 1609 is a pharmalogical agent with a favorable clinical safety profile and potential antiarrhythmic efficacy. It is used for the treatment of atrial fibrillation.
Storage
-20°C Freezer
Solubility
10 mM in DMSO
Shelf Life
2 month in rt, long time
Related Gap Junction Protein Products
  • CAS 943134-39-2 ZP 1609

    ZP 1609
    (CAS: 943134-39-2)

    ZP 1609, a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. It is a ph...

  • ZP 1609 Hydrochloride
    (CAS: 943133-81-1)

    ZP 1609 Hydrochloride is the hydrochloride form of ZP 1609, which is a small modified dipeptide and has been identified as a potent and selective second generat...

Reference Reading
1.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.
Butera JA1, Larsen BD, Hennan JK, Kerns E, Di L, Alimardanov A, Swillo RE, Morgan GA, Liu K, Wang Q, Rossman EI, Unwalla R, McDonald L, Huselton C, Petersen JS. J Med Chem. 2009 Feb 26;52(4):908-11. doi: 10.1021/jm801558d.
Rotigaptide (3) is an antiarrhythmic peptide that improves cardiac conduction by modifying gap-junction communication. Small molecule gap-junction modifiers with improved physical properties were identified from a Zealand Pharma peptide library using pharmaceutical profiling, established SAR around 3, and a putative pharmacophore model for rotigaptide. Activity of the compounds was confirmed in a mouse cardiac conduction block model of arrhythmia. Dipeptide 9f (GAP-134) was identified as a potent, orally active gap-junction modifier for clinical development.
2.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.
Hennan JK1, Swillo RE, Morgan GA, Rossman EI, Kantrowitz J, Butera J, Petersen JS, Gardell SJ, Vlasuk GP. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14. doi: 10.1177/1074248409340779.
The antiarrhythmic dipeptide, GAP-134, ([2S,4R]-1[2-aminoacetyl]-4-benzamido-pyrrolidine-2-carboxylic acid) was evaluated in canine ischemia/reperfusion model. In dogs subjected to 60-minute ischemia and 4-hour reperfusion, GAP-134 was administered 10 minutes before reperfusion as a bolus + intravenous (IV) infusion. The doses administered were 0.25 microg/kg bolus + 0.19 microg/kg per hour infusion; 2.5 microg/kg + 1.9 microg/kg per hour; 25 mg/kg + 19 mg/kg per hour; 75 mg/kg + 57 mg/kg per hour. Ventricular ectopy was quantified during reperfusion, including premature ventricular contractions (PVC) and ventricular tachycardia (VT). Total incidence of VT was reduced significantly with the 2 highest doses of GAP-134 (1.7 + 0.8; 2.2 + 1.4 events; P < .05) compared to controls (23.0 + 6.1). Total PVCs were reduced significantly from 11.1 + 1.6% in control animals to 2.0% + 0.7% and 1.8% + 0.8% after the 2 highest doses of GAP-134. Infarct size, expressed as percentage of left ventricle, was reduced significantly from 19.
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