PD-118057 | CAS#313674-97-4 | hERG channel enhancer

PD-118057
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561213

CAS#: 313674-97-4

Description: PD-118057 is a hERG channel enhancer. Human ether-a-go-go-related gene 1 (hERG1) K(+) channels mediate repolarization of cardiac action potentials.

Chemical Structure

PD-118057

CAS# 313674-97-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561213
Name: PD-118057
CAS#: 313674-97-4
Chemical Formula: C21H17Cl2NO2
Exact Mass: 385.06
Molecular Weight: 386.272
Elemental Analysis: C, 65.30; H, 4.44; Cl, 18.35; N, 3.63; O, 8.28

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 330
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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.

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

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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. Print 2013. PubMed PMID: 23840331; PubMed Central PMCID: PMC3686757.

2: 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. PubMed PMID: 19892732; PubMed Central PMCID: PMC2785294.

3: 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. PubMed PMID: 24638994; PubMed Central PMCID: PMC3971662.

4: 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. Epub 2005 Jun 23. PubMed PMID: 15976038.

5: 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. PubMed PMID: 18362027; PubMed Central PMCID: PMC2361425.

6: 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. PubMed PMID: 20042373; PubMed Central PMCID: PMC2826201.

7: 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. Epub 2006 Jul 26. PubMed PMID: 16870833.

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. PubMed PMID: 20876384; PubMed Central PMCID: PMC3014275.

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