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ChemicalBook--->CAS DataBase List--->353262-04-1

353262-04-1

353262-04-1 Structure

353262-04-1 Structure
IdentificationBack Directory
[Name]

NS-6180
[CAS]

353262-04-1
[Synonyms]

NS6180
NS-6180
NS 6180
CS-1648
NS6180 >=98% (HPLC)
NS6180;NS-6180;NS 6180
4-[[3-(Trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one
2H-1,4-Benzothiazin-3(4H)-one, 4-[[3-(trifluoromethyl)phenyl]methyl]-
[Molecular Formula]

C16H12F3NOS
[MOL File]

353262-04-1.mol
[Molecular Weight]

323.33
Chemical PropertiesBack Directory
[Boiling point ]

476.9±45.0 °C(Predicted)
[density ]

1.375±0.06 g/cm3(Predicted)
[storage temp. ]

Sealed in dry,2-8°C
[solubility ]

DMSO: soluble20mg/mL, clear
[form ]

powder
[pka]

0.53±0.20(Predicted)
[color ]

white to beige
Safety DataBack Directory
[Hazard Codes ]

Xi,N
[Risk Statements ]

43-51/53
[Safety Statements ]

61
[RIDADR ]

UN 3077 9 / PGIII
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

NS 6180 increases the proliferation of both A-NK and NA-NK cells. NS 6180 is a new KCa3.1 channel inhibitor that prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease.
[Biological Activity]

ns 6180 is a potent kca3.1 channel blocker. kca3.1 (the ca2+-activated k+ channel, encoded by the kcnn4 gene) plays a key role in these processes by participating in the regulation of calcium entry.
[in vitro]

ns6180 blocked cloned human kca3.1 channels via t250 and v275, while the same amino acid residues conferred sensitivity to triarylmethanes such as like tram-34. ns6180 blocked endogenously expressed kca3.1 channels in human, mouse and rat erythrocytes with similar potencies. rat and mouse splenocyte proliferation was suppressed ns6180 at submicrolar concentrations, which potently inhibited il-2 and ifn-g production, exerting smaller effects on il-4 and tnf-a and no effect on il-17 production. after induction of colitis, antibody staining exhibited kca3.1 channels in healthy colon and strong up-regulation in association with infiltrating immune cells [1].
[in vivo]

despite poor plasma exposure, ns6180 (3 and 10 mg·kg-1 b.i.d.) abolished colon inflammation and improved body weight gain effectively, just as the standard ibd drug sulfasalazine (300 mg·kg-1 q.d.). the benzothiazinone ns6180 was potent on recombinant and endogenously expressed kca3.1 channels, selectivity and molecular site of action. furthermore, the effect of ns6180 characterize its pharmacokinetics on the activity of t-lymphocytes from wild-type and kca3.1–/– knockout mice and show that it abolishes inflammation in an animal model of ibd [1].
[IC 50]

9, 14 and 15 nm for rat, human and mouse erythrocyte kca3.1 channels, respectively.
[storage]

Store at -20°C
[References]

[1] strbk d, brown dt, jenkins dp, chen yj, coleman n, ando y, chiu p, jrgensen s, demnitz j, wulff h, christophersen p. 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.
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