NS-1643
Modify Date: 2024-01-02 15:58:38
NS-1643 structure
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Common Name | NS-1643 | ||
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| CAS Number | 448895-37-2 | Molecular Weight | 380.24200 | |
| Density | 1.627g/cm3 | Boiling Point | 342.311ºC at 760 mmHg | |
| Molecular Formula | C15H10F6N2O3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 160.824ºC | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of NS-1643NS1643 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]. |
| Name | 1,3-bis[2-hydroxy-5-(trifluoromethyl)phenyl]urea |
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| Synonym | More Synonyms |
| 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 |
|---|---|
| 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 of Characters | white solid |
| Index of Refraction | 1.589 |
| Storage condition | -20℃ |
| Symbol |
GHS06 |
|---|---|
| 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 |
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The human ether-a-go-go-related gene activator NS1643 enhances epilepsy-associated KCNQ channels.
J. Pharmacol. Exp. Ther. , (2014) Human ether-a-go-go-related gene (hERG) and KCNQ channels are two classes of voltage-gated potassium channels. Specific mutations have been identified that are causal for type II long QT (LQT2) syndro... |
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Hydroxymethylation of microRNA-365-3p Regulates Nociceptive Behaviors via Kcnh2.
J. Neurosci. 36 , 2769-81, (2016) DNA 5-hydroxylmethylcytosine (5hmC) catalyzed by ten-eleven translocation methylcytosine dioxygenase (TET) occurs abundantly in neurons of mammals. However, the in vivo causal link between TET dysregu... |
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Potassium channel activation inhibits proliferation of breast cancer cells by activating a senescence program.
Cell Death Dis. 4 , e652, (2013) Traditionally the hERG1 potassium channel has been known to have a fundamental role in membrane excitability of several mammalian cells including cardiac myocytes. hERG1 has recently been found to be ... |
| ns1643 |
| NS-1643 |