CAS 448895-37-2|NS-1643

Introduction：Basic information about CAS 448895-37-2|NS-1643, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. NS-1643 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles3
6. Synonyms

Common Name	NS-1643
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	/
MSDS	ChineseUSA	Flash Point	160.824ºC
Symbol	GHS06	Signal Word	Danger

Names

Name	1,3-bis[2-hydroxy-5-(trifluoromethyl)phenyl]urea
Synonym	More Synonyms

NS-1643 BiologicalActivity

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].
Related Catalog	Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Others
References	[1]. Casis O, et al. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006 Feb;69(2):658-65. [2]. Hansen RS, et al. Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643). Mol Pharmacol. 2006 Jan;69(1):266-77. [3]. Elmedyb P, et al. Activation of ERG2 potassium channels by the diphenylurea NS1643. Neuropharmacology. 2007 Aug;53(2):283-94.

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].

Related Catalog

Signaling Pathways >>Autophagy >>AutophagySignaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Others

References

[1]. Casis O, et al. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006 Feb;69(2):658-65.

[2]. Hansen RS, et al. Activation of human ether-a-go-go-related gene potassium channels by the diphenylurea 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643). Mol Pharmacol. 2006 Jan;69(1):266-77.

[3]. Elmedyb P, et al. Activation of ERG2 potassium channels by the diphenylurea NS1643. Neuropharmacology. 2007 Aug;53(2):283-94.

Chemical & Physical Properties

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
InChIKey	NJFVQMRYJZHGME-UHFFFAOYSA-N
SMILES	O=C(Nc1cc(C(F)(F)F)ccc1O)Nc1cc(C(F)(F)F)ccc1O
Storage condition	-20℃

Safety Information

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

Articles3

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...

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...

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 ...

Synonyms

ns1643

NS-1643

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