Name | 1,3-bis[2-hydroxy-5-(trifluoromethyl)phenyl]urea |
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Synonyms |
ns1643
NS-1643 |
Description | NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator (EC50 = 10.5 μM).IC50 value:Target: HERG activatorin vitro: NS1643 enhanced the magnitude of wild-type hERG current in a concentration- and voltage-dependent manner with an EC(50) of 10.4 microM at -10 mV. The fully activated current-voltage relationship revealed that the drug increased outward but not inward currents, consistent with altered inactivation gating. NS1643 shifted the voltage dependence of inactivation by +21 mV at 10 microM and +35 mV at 30 microM, but it did not alter the voltage dependence of activation of hERG channels [1]. In Xenopus laevis oocytes, NS1643 increased both steady-state and tail current at all voltages tested. The EC(50) value for HERG channel activation was 10.5 microM [2]. NS1643 also activates the ERG2 channel; however, the molecular mechanism of the activation differs between the ERG1 and ERG2 channels. For ERG2, NS1643 causes a left-ward shift of the activation curve, a faster time-constant of activation and a slower time-constant of inactivation as well as an increased relative importance for the fast component of deactivation to the total deactivation. In contrast, for ERG1, NS1643 causes a right-ward shift in the voltage-dependent release from inactivation but does not affect time-constants of deactivation [3]. |
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Related Catalog | |
References |
Density | 1.627g/cm3 |
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Boiling Point | 342.311ºC at 760 mmHg |
Molecular Formula | C15H10F6N2O3 |
Molecular Weight | 380.24200 |
Flash Point | 160.824ºC |
Exact Mass | 380.06000 |
PSA | 81.59000 |
LogP | 4.92540 |
Appearance | white solid |
Index of Refraction | 1.589 |
Storage condition | -20℃ |
Symbol |
![]() GHS06 |
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Signal Word | Danger |
Hazard Statements | H301-H319 |
Precautionary Statements | P301 + P310-P305 + P351 + P338 |
Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Faceshields;Gloves |
RIDADR | UN 2811 6.1 / PGIII |