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  • DC Chemicals Limited
  • China
  • Product Name: NS6180
  • Price: $300.0/100mg $600.0/250mg $1200.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

353262-04-1

353262-04-1 structure
353262-04-1 structure
  • Name: NS 6180
  • Chemical Name: 4-[3-(Trifluoromethyl)benzyl]-2H-1,4-benzothiazin-3(4H)-one
  • CAS Number: 353262-04-1
  • Molecular Formula: C16H12F3NOS
  • Molecular Weight: 323.333
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
  • Create Date: 2019-01-02 15:48:07
  • Modify Date: 2024-01-02 18:48:59
  • 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].

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

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
Storage condition 2-8℃
Symbol GHS07 GHS09
GHS07, GHS09
Signal Word Warning
Hazard Statements H317-H411
Precautionary Statements P273-P280
RIDADR UN 3077 9 / PGIII