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PD-118057

Cat. No. M8016

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PD-118057 Structure

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Quality Control & Documentation
Biological Activity

PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activator, a representative in the series of structural analogs; PD-118057 at 10 μM leads to a 111% current increase in rabbit ventricular wedge (in comparison RPR260243 leads to only a 15% increase at the same concentration);PD-118057, unlike RPR260243, does not have a major effect on gating or kinetic properties of this channel. PD-118057prevents and reverses QT interval prolongation; Compounds such as PD-118057 may offer new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure

Chemical Information
Molecular Weight 386.27
Formula C21H17Cl2NO2
CAS Number 313674-97-4
Solubility (25°C) DMSO: 9 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wei Wu, et al. Stoichiometry of altered hERG1 channel gating by small molecule activators

[2] Haiyan Mao, et al. Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin

[3] Eyal Nof, et al. Cellular basis for atrial fibrillation in an experimental model of short QT1: implications for a pharmacological approach to therapy

[4] Matthew Perry, et al. PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K+ conductance

[5] Jun Zhou, et al. Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity

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Keywords: PD-118057 supplier, inhibitors, activators

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