| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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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