azo-Q2a
azo-Q2a is a photoswitchable NaV1.5 inhibitor. azo-Q2a exists as the trans isomer with low activity in the dark or under 480 nm illumination, and exists as the cis isomer with higher inhibitory potency under 365 nm illumination. azo-Q2a reduces the heart rate of living zebrafish larvae in a light-dependent manner. azo-Q2a can be used for the study of arrhythmias.
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- Fòrmula: C32H32N4O2
- Peso molecular:504.62
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Almacenamiento:
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Actividad biológica
Azo-Q2a (10 μM; during patch-clamp recordings) enables reversible, light-dependent inhibition of NaV1.5 channels in HEK293T cells, with cis-azo-Q2a formed under 365 nm illumination showing 7-fold higher potency, with an IC50 of 11.76 μM, than trans-azo-Q2a from dark/480 nm illumination, which has an IC50 of 81.58 μM, without altering channel activation[1].
Azo-Q2a (10 μM; during patch-clamp recordings) exhibits high light-dependent selectivity for NaV1.5 over other NaV subtypes and cardiac ion channels in HEK293T and CHO cells, with cis-azo-Q2a formed under 365 nm illumination showing significantly reduced hERG inhibition relative to quinidine[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Azo-Q2a (10 μM; administered after tachycardia induction; 365 nm light irradiation for 5 min (cis isomer); dark incubation (trans isomer)) effectively terminates isoproterenol-induced tachycardia in zebrafish larvae when activated to its cis isomer by 365 nm light, reducing the heart rate to 35.3% of the baseline level, whereas the trans isomer in dark conditions exerts only a very weak effect[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AB strain (2 days post-fertilization larvae, gender not screened)[1]
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Dosage:10 μM
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Administration:soaked; dark incubation for 1-1.5 h
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Result:Had no significant effect on heart rate, with values measured at 98.8% of control baseline.
Reduced heart rate significantly to 56.5% of baseline after 365 nm illumination.
Restored heart rate to 103.2% of baseline after subsequent 480 nm illumination.
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Animal Model:AB strain (3-4 days post-fertilization larvae, gender not screened)[1]
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Dosage:10 μM
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Administration:applied after tachycardia induction; 365 nm illumination for 5 min (cis isomer); dark incubation (trans isomer)
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Result:Markedly attenuated tachycardic heart rate to 35.3% of baseline under 365 nm illumination (cis isomer).
Produced only a mild 4.4% reduction in tachycardic heart rate in the dark (trans isomer).
Chemical Information
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Peso molecular 504.62
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Fòrmula C32H32N4O2
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SMILES
COC1=CC2=C(N=CC(C3=CC=C(C=C3)/N=N/C4=CC=CC=C4)=C2[C@@H]([C@@H]5[N@](C[C@@H]6C=C)CC[C@H]6C5)O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
azo-Q2a Related Classifications
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