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GAP-134 Hydrochloride

Gap-junction modifier,potent and selective CAS# 943133-81-1

GAP-134 Hydrochloride

Catalog No. BCC1589----Order now to get a substantial discount!

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GAP-134 Hydrochloride: 5mg $334 In Stock
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Quality Control of GAP-134 Hydrochloride

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Chemical structure

GAP-134 Hydrochloride

3D structure

Chemical Properties of GAP-134 Hydrochloride

Cas No. 943133-81-1 SDF Download SDF
PubChem ID 44563896 Appearance Powder
Formula C14H18ClN3O4 M.Wt 327.76
Type of Compound N/A Storage Desiccate at -20°C
Synonyms Danegaptide Hydrochloride; ZP 1609 Hydrochloride
Solubility H2O : ≥ 75 mg/mL (228.83 mM)
DMSO : ≥ 55 mg/mL (167.81 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid;hydrochloride
SMILES C1C(CN(C1C(=O)O)C(=O)CN)NC(=O)C2=CC=CC=C2.Cl
Standard InChIKey AHXPMNACLWKFRQ-DHXVBOOMSA-N
Standard InChI InChI=1S/C14H17N3O4.ClH/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);1H/t10-,11+;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GAP-134 Hydrochloride

DescriptionGAP-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:
[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

GAP-134 Hydrochloride Dilution Calculator

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GAP-134 Hydrochloride Molarity Calculator

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Preparing Stock Solutions of GAP-134 Hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.051 mL 15.2551 mL 30.5101 mL 61.0203 mL 76.2753 mL
5 mM 0.6102 mL 3.051 mL 6.102 mL 12.2041 mL 15.2551 mL
10 mM 0.3051 mL 1.5255 mL 3.051 mL 6.102 mL 7.6275 mL
50 mM 0.061 mL 0.3051 mL 0.6102 mL 1.2204 mL 1.5255 mL
100 mM 0.0305 mL 0.1526 mL 0.3051 mL 0.6102 mL 0.7628 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GAP-134 Hydrochloride

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-134 (Danegaptide), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability. 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.

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References on GAP-134 Hydrochloride

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.[Pubmed:19175320]

J Med Chem. 2009 Feb 26;52(4):908-11.

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.

Description

Danegaptide Hydrochloride (GAP-134 Hydrochloride) is a selective modifier of the gap junction protein.

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