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MedKoo Cat#: 561213 | Name: PD-118057
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PD-118057 is a hERG channel enhancer. Human ether-a-go-go-related gene 1 (hERG1) K(+) channels mediate repolarization of cardiac action potentials. PD-118057 alters selectivity filter gating to enhance open probability of K+ channels.

Chemical Structure

PD-118057
PD-118057
CAS#313674-97-4

Theoretical Analysis

MedKoo Cat#: 561213

Name: PD-118057

CAS#: 313674-97-4

Chemical Formula: C21H17Cl2NO2

Exact Mass: 385.0636

Molecular Weight: 386.27

Elemental Analysis: C, 65.30; H, 4.44; Cl, 18.35; N, 3.63; O, 8.28

Price and Availability

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5mg USD 550.00
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Synonym
PD-118057; PD118057; PD 118057
IUPAC/Chemical Name
2-[4-[2-(3,4-Dichlorophenyl)ethyl]anilino]benzoic acid
InChi Key
ZCQOSCDABPVAFB-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H17Cl2NO2/c22-18-12-9-15(13-19(18)23)6-5-14-7-10-16(11-8-14)24-20-4-2-1-3-17(20)21(25)26/h1-4,7-13,24H,5-6H2,(H,25,26)
SMILES Code
O=C(O)C1=CC=CC=C1NC2=CC=C(CCC3=CC=C(Cl)C(Cl)=C3)C=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PD-118057 is a hERG channel activator without causing hERG blockade.
In vitro activity:
In this study, PD-118057 was shown to significantly enhance both the maximum current amplitude and tail current amplitude, but did not alter the gating and kinetic properties of the WT-hERG channel, with the exception of accelerating steady-state inactivation. Additionally, thapsigargin shows a similar result as PD-118057 for the WT-hERG channel, but with the exception of attenuating steady-state inactivation. Reference: PLoS One. 2013 Jun 19;8(6):e65481. https://pubmed.ncbi.nlm.nih.gov/23840331/
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 386.27 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Mao H, Lu X, Karush JM, Huang X, Yang X, Ba Y, Wang Y, Liu N, Zhou J, Lian J. Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. PLoS One. 2013 Jun 19;8(6):e65481. doi: 10.1371/journal.pone.0065481. PMID: 23840331; PMCID: PMC3686757. 2. Yeung SY, Greenwood IA. Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells. Am J Physiol Cell Physiol. 2007 Jan;292(1):C468-76. doi: 10.1152/ajpcell.00142.2006. Epub 2006 Jul 26. PMID: 16870833.
In vitro protocol:
1. Mao H, Lu X, Karush JM, Huang X, Yang X, Ba Y, Wang Y, Liu N, Zhou J, Lian J. Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. PLoS One. 2013 Jun 19;8(6):e65481. doi: 10.1371/journal.pone.0065481. PMID: 23840331; PMCID: PMC3686757. 2. Yeung SY, Greenwood IA. Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells. Am J Physiol Cell Physiol. 2007 Jan;292(1):C468-76. doi: 10.1152/ajpcell.00142.2006. Epub 2006 Jul 26. PMID: 16870833.
In vivo protocol:
TBD
1: Park NK, Park SJ, Park YG, Moon SH, Woo J, Kim HJ, Kim SJ, Choi SW. 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. Hum Mol Genet. 2024 Jan 7;33(2):110-121. doi: 10.1093/hmg/ddad165. PMID: 37769355. 2: Hull CM, Genge CE, Hobbs Y, Rayani K, Lin E, Gunawan M, Shafaattalab S, Tibbits GF, Claydon TW. Investigating the utility of adult zebrafish ex vivo whole hearts to pharmacologically screen hERG channel activator compounds. Am J Physiol Regul Integr Comp Physiol. 2019 Dec 1;317(6):R921-R931. doi: 10.1152/ajpregu.00190.2019. Epub 2019 Oct 30. PMID: 31664867; PMCID: PMC6962622. 3: Schewe M, Sun H, Mert Ü, Mackenzie A, Pike ACW, Schulz F, Constantin C, Vowinkel KS, Conrad LJ, Kiper AK, Gonzalez W, Musinszki M, Tegtmeier M, Pryde DC, Belabed H, Nazare M, de Groot BL, Decher N, Fakler B, Carpenter EP, Tucker SJ, Baukrowitz T. A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels. Science. 2019 Feb 22;363(6429):875-880. doi: 10.1126/science.aav0569. PMID: 30792303; PMCID: PMC6982535. 4: So EC, Foo NP, Ko SY, Wu SN. Bisoprolol, Known to Be a Selective β₁-Receptor Antagonist, Differentially but Directly Suppresses IK(M) and IK(erg) in Pituitary Cells and Hippocampal Neurons. Int J Mol Sci. 2019 Feb 2;20(3):657. doi: 10.3390/ijms20030657. PMID: 30717422; PMCID: PMC6386942. 5: Donovan BT, Bandyopadhyay D, Duraiswami C, Nixon CJ, Townsend CY, Martens SF. Discovery and electrophysiological characterization of SKF-32802: A novel hERG agonist found through a large-scale structural similarity search. Eur J Pharmacol. 2018 Jan 5;818:306-327. doi: 10.1016/j.ejphar.2017.10.015. Epub 2017 Oct 16. PMID: 29050968. 6: Wu W, Sachse FB, Gardner A, Sanguinetti MC. Stoichiometry of altered hERG1 channel gating by small molecule activators. J Gen Physiol. 2014 Apr;143(4):499-512. doi: 10.1085/jgp.201311038. Epub 2014 Mar 17. PMID: 24638994; PMCID: PMC3971662. 7: Mao H, Lu X, Karush JM, Huang X, Yang X, Ba Y, Wang Y, Liu N, Zhou J, Lian J. Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. PLoS One. 2013 Jun 19;8(6):e65481. doi: 10.1371/journal.pone.0065481. PMID: 23840331; PMCID: PMC3686757. 8: Grunnet M, Abbruzzese J, Sachse FB, Sanguinetti MC. Molecular determinants of human ether-à-go-go-related gene 1 (hERG1) K+ channel activation by NS1643. Mol Pharmacol. 2011 Jan;79(1):1-9. doi: 10.1124/mol.110.067728. Epub 2010 Sep 27. PMID: 20876384; PMCID: PMC3014275. 9: Lazzara R. How the heart can fibrillate: when diversity is a disadvantage. Heart Rhythm. 2010;7(2):258-9. doi: 10.1016/j.hrthm.2009.10.033. Epub 2009 Oct 30. PMID: 20129301. 10: Nof E, Burashnikov A, Antzelevitch C. Cellular basis for atrial fibrillation in an experimental model of short QT1: implications for a pharmacological approach to therapy. Heart Rhythm. 2010;7(2):251-7. doi: 10.1016/j.hrthm.2009.10.017. Epub 2009 Oct 17. PMID: 20042373; PMCID: PMC2826201. 11: Perry M, Sachse FB, Abbruzzese J, Sanguinetti MC. PD-118057 contacts the pore helix of hERG1 channels to attenuate inactivation and enhance K+ conductance. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20075-80. doi: 10.1073/pnas.0906597106. Epub 2009 Nov 5. PMID: 19892732; PMCID: PMC2785294. 12: Greenwood IA, Yeung SY, Tribe RM, Ohya S. Loss of functional K+ channels encoded by ether-à-go-go-related genes in mouse myometrium prior to labour onset. J Physiol. 2009 May 15;587(Pt 10):2313-26. doi: 10.1113/jphysiol.2009.171272. Epub 2009 Mar 30. PMID: 19332483; PMCID: PMC2697300. 13: Duff HJ. hERG: the long and short of it. Heart Rhythm. 2008 Apr;5(4):591-2. doi: 10.1016/j.hrthm.2008.02.041. Epub 2008 Mar 6. PMID: 18362028. 14: Patel C, Antzelevitch C. Cellular basis for arrhythmogenesis in an experimental model of the SQT1 form of the short QT syndrome. Heart Rhythm. 2008 Apr;5(4):585-90. doi: 10.1016/j.hrthm.2008.01.022. Epub 2008 Jan 29. PMID: 18362027; PMCID: PMC2361425. 15: Yeung SY, Greenwood IA. Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells. Am J Physiol Cell Physiol. 2007 Jan;292(1):C468-76. doi: 10.1152/ajpcell.00142.2006. Epub 2006 Jul 26. PMID: 16870833. 16: Zhou J, Augelli-Szafran CE, Bradley JA, Chen X, Koci BJ, Volberg WA, Sun Z, Cordes JS. Novel potent human ether-a-go-go-related gene (hERG) potassium channel enhancers and their in vitro antiarrhythmic activity. Mol Pharmacol. 2005 Sep;68(3):876-84. doi: 10.1124/mol.105.014035. Epub 2005 Jun 23. PMID: 15976038.