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KB130015

Cat. No. M28509
KB130015 Structure
Synonym:

KB015

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Quality Control & Documentation
Biological Activity

KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle.

Chemical Information
Molecular Weight 548.11
Formula C18H14I2O4
CAS Number 147030-48-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Guido Gessner, et al. Eur J Pharmacol. The amiodarone derivative KB130015 activates hERG1 potassium channels via a novel mechanism

[2] Guido Gessner, et al. Eur J Pharmacol. The amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015) opens large-conductance Ca2+-activated K+ channels and relaxes vascular smooth muscle

[3] B Brandts, et al. J Pharmacol Exp Ther. Inhibition of G protein-coupled and ATP-sensitive potassium currents by 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015), an amiodarone derivative

[4] Kanigula Mubagwa, et al. Cardiovasc Drug Rev. KB130015, a new amiodarone derivative with multiple effects on cardiac ion channels

[5] R Macianskiene, et al. J Pharmacol Exp Ther. Slowing of the inactivation of cardiac voltage-dependent sodium channels by the amiodarone derivative 2-methyl-3-(3,5-diiodo-4-carboxymethoxybenzyl)benzofuran (KB130015)

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  Catalog
Abmole Inhibitor Catalog




Keywords: KB130015, KB015 supplier, Thyroid Hormone Receptor, inhibitors, activators


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