Molecular structure of PD-118057, CAS Number: 313674-97-4
PD-118057 (CAS 313674-97-4)
Alternate Names:
2-[[4-[2-(3,4-Dichlorophenyl)ethyl]phenyl]amino]benzoic acid
Application:
PD-118057 is an activator of HERG (ether-a-go-go-related (hERG) potassium channel)
CAS Number:
313674-97-4
Molecular Weight:
386.27
Molecular Formula:
C21H17Cl2NO2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
An activator of ether-a-go-go-related (hERG) potassium channel. It 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. This chemical prevents and reverses QT interval prolongation. Compounds such as PD-118057 may offer a new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure.
PD-118057 (CAS 313674-97-4) References
- Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. | Zhou, J., et al. 2005. Mol Pharmacol. 68: 876-84. PMID: 15976038
- PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K+ conductance. | Perry, M., et al. 2009. Proc Natl Acad Sci U S A. 106: 20075-80. PMID: 19892732
- Cellular basis for atrial fibrillation in an experimental model of short QT1: implications for a pharmacological approach to therapy. | Nof, E., et al. 2010. Heart Rhythm. 7: 251-7. PMID: 20042373
- Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. | Mao, H., et al. 2013. PLoS One. 8: e65481. PMID: 23840331
- Antiarrhythmics cure brain arrhythmia: The imperativeness of subthalamic ERG K+ channels in parkinsonian discharges. | Huang, CS., et al. 2017. Sci Adv. 3: e1602272. PMID: 28508055
- Proliferative Role of Kv11 Channels in Murine Arteries. | Barrese, V., et al. 2017. Front Physiol. 8: 500. PMID: 28747891
- Bisoprolol, Known to Be a Selective β₁-Receptor Antagonist, Differentially but Directly Suppresses IK(M) and IK(erg) in Pituitary Cells and Hippocampal Neurons. | So, EC., et al. 2019. Int J Mol Sci. 20: PMID: 30717422
- A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels. | Schewe, M., et al. 2019. Science. 363: 875-880. PMID: 30792303
- Evidence for Effective Multiple K+-Current Inhibitions by Tolvaptan, a Non-peptide Antagonist of Vasopressin V2 Receptor. | Lu, TL., et al. 2019. Front Pharmacol. 10: 76. PMID: 30873020
- Investigating the utility of adult zebrafish ex vivo whole hearts to pharmacologically screen hERG channel activator compounds. | Hull, CM., et al. 2019. Am J Physiol Regul Integr Comp Physiol. 317: R921-R931. PMID: 31664867
- Evidence for the Capability of Roxadustat (FG-4592), an Oral HIF Prolyl-Hydroxylase Inhibitor, to Perturb Membrane Ionic Currents: An Unidentified yet Important Action. | Chang, WT., et al. 2019. Int J Mol Sci. 20: PMID: 31795416
- An Update on the Structure of hERG. | Butler, A., et al. 2019. Front Pharmacol. 10: 1572. PMID: 32038248
- Translation reinitiation in c.453delC frameshift mutation of KCNH2 producing functional hERG K+ channels with mild dominant negative effect in the heterozygote patient-derived iPSC cardiomyocytes. | Park, NK., et al. 2024. Hum Mol Genet. 33: 110-121. PMID: 37769355
Inhibitor of:
EAG, GPR176, and KV4.3.Activator of:
HERG, KCNQ5, KCNV1, KIR2.4, and P/Q-type Ca++ CP α1A.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PD-118057, 5 mg | sc-253238 | 5 mg | $215.00 |