CAS 353262-04-1|NS 6180

Introduction：Basic information about CAS 353262-04-1|NS 6180, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. NS 6180 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	NS 6180
CAS Number	353262-04-1	Molecular Weight	323.333
Density	1.4±0.1 g/cm3	Boiling Point	476.9±45.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₂F₃NOS	Melting Point	/
MSDS	ChineseUSA	Flash Point	242.2±28.7 °C
Symbol	GHS07, GHS09	Signal Word	Warning

Names

Name	4-[3-(Trifluoromethyl)benzyl]-2H-1,4-benzothiazin-3(4H)-one
Synonym	More Synonyms

NS 6180 BiologicalActivity

Description	NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.IC50 value: 9 nM [1]Target: KCa3.1 channel inhibitorin vitro: NS6180 inhibited cloned human KCa3.1 channels (IC50 = 9 nM) via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM). NS6180 suppressed rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-γ production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production [1].in vivo: DNBS challenged rats were treated with two doses (3 and 10 mg·kg-1 b.i.d.) of NS6180 for 7 days in direct comparison with the IBD drug sulfasalazine (300 mg·kg-1 q.d.). Both doses of NS6180 significantly improved weight gain and decreased inflammation induced swelling of the colon as determined by relative colon weight [1].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Inflammation/Immunology
References	[1]. Strobak D, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44. [2]. Jorgensen S, et al. A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol. 2013 Apr;11(3):163-72.

Description

NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.IC50 value: 9 nM [1]Target: KCa3.1 channel inhibitorin vitro: NS6180 inhibited cloned human KCa3.1 channels (IC50 = 9 nM) via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM). NS6180 suppressed rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-γ production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production [1].in vivo: DNBS challenged rats were treated with two doses (3 and 10 mg·kg-1 b.i.d.) of NS6180 for 7 days in direct comparison with the IBD drug sulfasalazine (300 mg·kg-1 q.d.). Both doses of NS6180 significantly improved weight gain and decreased inflammation induced swelling of the colon as determined by relative colon weight [1].

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Inflammation/Immunology

References

[1]. Strobak D, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44.

[2]. Jorgensen S, et al. A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol. 2013 Apr;11(3):163-72.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	476.9±45.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₂F₃NOS
Molecular Weight	323.333
Flash Point	242.2±28.7 °C
Exact Mass	323.059174
PSA	45.61000
LogP	3.89
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.594
InChIKey	ZUIJXKLTUFCDGO-UHFFFAOYSA-N
SMILES	O=C1CSc2ccccc2N1Cc1cccc(C(F)(F)F)c1
Storage condition	2-8℃

Safety Information

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H317-H411
Precautionary Statements	P273-P280
RIDADR	UN 3077 9 / PGIII

Synonyms

2H-1,4-Benzothiazin-3(4H)-one, 4-[[3-(trifluoromethyl)phenyl]methyl]-

4-[3-(Trifluoromethyl)benzyl]-2H-1,4-benzothiazin-3(4H)-one

NS6180

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