| Identification | Back Directory | [Name]
PD-118057 | [CAS]
313674-97-4 | [Synonyms]
PD-118057 >=98% (HPLC), solid
Benzoic acid, 2-[[4-[2-(3,4-dichlorophenyl)ethyl]phenyl]amino]- | [Molecular Formula]
C21H17Cl2NO2 | [MDL Number]
MFCD08705328 | [MOL File]
313674-97-4.mol | [Molecular Weight]
386.27 |
| Chemical Properties | Back Directory | [Boiling point ]
527.0±50.0 °C(Predicted) | [density ]
1.353±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble9mg/mL | [form ]
solid | [pka]
3.70±0.36(Predicted) | [color ]
light yellow | [InChI]
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) | [InChIKey]
ZCQOSCDABPVAFB-UHFFFAOYSA-N | [SMILES]
C(O)(=O)C1=CC=CC=C1NC1=CC=C(CCC2=CC=C(Cl)C(Cl)=C2)C=C1 |
| Hazard Information | Back Directory | [Uses]
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability[1][2]. | [Biological Activity]
PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activatora 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-118057unlike RPR260243does 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 conditionswhich occur in inherited or acquired long QT syndrome and congestive heart failure | [References]
[1] Mao H, et al. 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
[2] Yeung SY, et al. 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
[3] Meng J, et al. Effect of PD-118057attenuates hypokalaemia or drug-induced prolongation of action potential duration in guinea pig ventricular myocytes. 2014,29(05):536-538. |
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