| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PA-6 targets the inward rectifier potassium current (IK1), which is mediated by Kir2.x potassium channels. By blocking IK1, PA-6 reduces the repolarization reserve of cardiac myocytes, making it a valuable tool for studying arrhythmogenesis. The compound's selective inhibition of IK1 without causing ventricular arrhythmias makes it a useful research tool for studying atrial fibrillation.
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| ln Vitro |
In vitro, PA-6 acts as a selective and potent inhibitor of IK1. It blocks Kir2.x channels, reducing the inward rectifier potassium current in cardiac myocytes. The compound's activity is typically assessed in electrophysiological studies using patch-clamp techniques to measure IK1 inhibition in isolated cardiac myocytes or heterologous expression systems.
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| ln Vivo |
In vivo, PA-6 terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. This demonstrates its potential as a selective anti-arrhythmic agent for atrial fibrillation without the pro-arrhythmic risk associated with non-selective potassium channel blockers. The compound's efficacy in large animal models supports its utility for studying IK1 in cardiac arrhythmias.
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| Enzyme Assay |
As a potassium channel inhibitor, PA-6 is not typically evaluated in cell-free receptor binding assays. Its activity is assessed by electrophysiological techniques measuring ion channel currents in cell-based systems. The compound's selectivity for Kir2.x channels over other potassium channels can be evaluated using patch-clamp recordings in cells expressing specific channel subtypes.
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| Cell Assay |
In vitro cell-based experiments with PA-6 typically involve electrophysiological studies using the patch-clamp technique. Cells expressing Kir2.x channels (e.g., HEK293 cells transfected with Kir2.1) or isolated cardiac myocytes are used. The compound is applied at various concentrations, and the inhibition of IK1 current is measured. The IC50 for IK1 inhibition is determined from concentration-response curves.
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| Animal Protocol |
In vivo animal experiments with PA-6 have been conducted in goat and dog models. In typical protocols, atrial fibrillation is induced in the animals, and PA-6 is administered intravenously. Electrocardiograms are recorded to monitor the termination of atrial fibrillation and the absence of ventricular arrhythmias. The compound's effects on cardiac electrophysiology are assessed.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for PA-6. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. The compound has a molecular formula of C31H32N4O2 and a molecular weight of 492.61.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for PA-6. In animal studies, the compound terminated atrial fibrillation without causing ventricular arrhythmias, suggesting a favorable cardiac safety profile. The compound is for research use only and is not intended for human therapeutic applications.
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| References |
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| Additional Infomation |
PA-6 has a molecular formula of C31H32N4O2 and a molecular weight of 492.61. Its IUPAC name is N,N''-((pentane-1,5-diylbis(oxy))bis(4,1-phenylene))dibenzimidamide. It is a selective and potent IK1 inhibitor that terminates atrial fibrillation in goat and dog models without causing ventricular arrhythmias. It is available for research purposes only.
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| Molecular Formula |
C31H32N4O2
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|---|---|
| Molecular Weight |
492.61138
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| Exact Mass |
492.252
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| CAS # |
500715-03-7
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| Related CAS # |
500715-03-7;
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| PubChem CID |
11752239
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
37
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| Complexity |
625
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OC1C=CC(NC(C2C=CC=CC=2)=N)=CC=1)CCCCOC1C=CC(NC(C2C=CC=CC=2)=N)=CC=1
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| InChi Key |
PETGITKEGWIZEL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H32N4O2/c32-30(24-10-4-1-5-11-24)34-26-14-18-28(19-15-26)36-22-8-3-9-23-37-29-20-16-27(17-21-29)35-31(33)25-12-6-2-7-13-25/h1-2,4-7,10-21H,3,8-9,22-23H2,(H2,32,34)(H2,33,35)
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| Chemical Name |
N'-[4-[5-[4-[[amino(phenyl)methylidene]amino]phenoxy]pentoxy]phenyl]benzenecarboximidamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~253.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0300 mL | 10.1500 mL | 20.3000 mL | |
| 5 mM | 0.4060 mL | 2.0300 mL | 4.0600 mL | |
| 10 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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