AZD-1305
AZD-1305 is an antiarrhythmic agent and atrial selective sodium channel/potassium channel blocker, which can significantly prolongs action potential duration and reduces excitability, cause atrial selective ERP prolongation and acute termination of atrial fibrillation. AZD1305 can be used for atrial fibrillation research.
For research use only. We do not sell to patients.
- CAS No.: 872045-91-5
- Formula: C22H31FN4O4
- Molecular Weight:434.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Calcium Channel Isoforms
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Biological Activity
Description
In Vitro
AZD-1305 (1,3 μM) induces atrial selective PRR in isolated coronary-perfused preparations [1].
AZD-1305 (1,3 μM) produces a greater use-dependent reduction of maximum rate of rise of the action potential upstroke (Vmax) in atrial versus ventricular preparations[1].
AZD-1305 (1,3 μM) causes a greater increase in sodium channel–mediated parameters conduction velocity and diastolic threshold of excitation in atrial versus ventricular coronaryperfused preparations[1].
AZD-1305 (5 μM) induces greater tonic and steadystate inhibitions of atrial sodium channels than ventricular sodium channels in isolated coronary-perfused preparations[1].
AZD-1305 (1-10 μM) causes a significant decrease in Vmax, action potential amplitude, and takeoff potential in canine pulmonary vein sleeve preparations, and significantly increases action potential duration at 90% repolarization[2].
AZD-1305 (1-10 μM) significantly increases the basic cycle length at which 1:1 activation is maintained in canine pulmonary vein sleeve preparations, and pretreatment with amiodarone significantly potentiates the effect of AZD1305[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
AZD-1305 (steady state plasma concentrations of 1.2 and 4.5 μM, i.v.drip) increases conduction time and depress excitability in atria versus ventricles of Beagle dogs [1].
AZD-1305 (steady state plasma concentrations of 1-3 μM, i.v.drip) terminates persistent AF and prevents induction of AF in an ACh-mediated model of AF in Beagle dogs [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 872045-91-5
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Molecular Weight 434.50
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Formula C22H31FN4O4
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SMILES
O=C(OC(C)(C)C)NCCN1CC(O2)CN(CCOC3=CC=C(C#N)C=C3F)CC2C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cardiac voltage-sensitive optical mapping
Cardiac voltage-sensitive optical mapping records changes in transmembrane potential from cardiac tissue by staining the preparation with a voltage-sensitive dye and imaging fluorescence changes during electrical activation; the resulting optical action potentials can be used to map activation time, action potential duration, conduction velocity, wavefront propagation, and arrhythmia dynamics. The optical signal represents a relative fluorescence change from a tissue volume rather than a single-cell intracellular recording, so spatial resolution, sampling rate, voltage resolution, optical magnification, light penetration, and motion control must be considered together when interpreting optical action potentials.
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
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Acute brain-slice whole-cell patch-clamp recording
Acute brain-slice whole-cell patch-clamp recording measures membrane voltage or ionic current from visually targeted cells in living brain slices; after giga-seal formation, the membrane under the pipette is ruptured to provide low-resistance electrical access to the cell interior, enabling current-clamp analysis of excitability and voltage-clamp analysis of synaptic or membrane currents. Acute slices preserve local tissue architecture better than dissociated preparations and allow visually guided recording from defined brain regions or fluorescently labeled cells; however, whole-cell access also permits exchange between pipette solution and cytoplasm, so intracellular dialysis must be considered when interpreting signaling-dependent phenomena.
Purity & Documentation
References
[1]. Charles Antzelevitch, et al. AZD1305 Exerts Atrial Predominant Electrophysiological Actions and Is Effective in Suppressing Atrial Fibrillation and Preventing Its Reinduction in the Dog. [J] Cardiovasc Pharmacol. 2010, Volume 56,Number 1. [Content Brief]
[2]. Serge Sicouri, et al. Electrophysiologic and antiarrhythmic effects of AZD1305 in canine pulmonary vein sleeves. THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. 2010, Volume 334,Number 1. [Content Brief]
[3]. Alexander Burashnikov, et al. AZD1305 exerts atrial predominant electrophysiological actions and is effective in suppressing atrial fibrillation and preventing its reinduction in the dog. J Cardiovasc Pharmacol. 2010 Jul;56(1):80-90. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)