GAP-134 HydrochlorideGap-junction modifier,potent and selective CAS# 943133-81-1 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| 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: | |||||
GAP-134 Hydrochloride Dilution Calculator
GAP-134 Hydrochloride Molarity Calculator
| 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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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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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.
