| Bioactivity | PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress changes in membrane excitability[1][2]. | |||||||||
| Target | Human ether-a-go-go-related gene channel | |||||||||
| Invitro | PD-118057 (3 μM and 10 μM) specifically increases hERG current and inhibits action potential duration in guinea pig ventricular muscle in acute isolation of guinea pig cardiomyocytes[2][3].PD-118057 (10 μM) reverses the current inhibition induced by Dof and Mox without changing the "hump" shape of IKr current recorded by action potential clamp, and only slightly increases the peak value of the suppressed current[3]. | |||||||||
| Name | PD-118057 | |||||||||
| CAS | 313674-97-4 | |||||||||
| Formula | C21H17Cl2NO2 | |||||||||
| Molar Mass | 386.27 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. [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. [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. |
PD-118057
CAS: 313674-97-4 F: C21H17Cl2NO2 W: 386.27
PD-118057 is a hERG channel activator without causing hERG blockade. PD-118057 activates hERG channel to suppress change
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