Name | NS6180 |
Synonyms | NS6180 NS-6180 CS-1648 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]- |
CAS | 353262-04-1 |
Molecular Formula | C16H12F3NOS |
Molar Mass | 323.33 |
Density | 1.375±0.06 g/cm3(Predicted) |
Boling Point | 476.9±45.0 °C(Predicted) |
Solubility | DMSO: ≥ 47 mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 0.53±0.20(Predicted) |
Storage Condition | Sealed in dry,2-8°C |
Risk Codes | R43 - May cause sensitization by skin contact R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.093 ml | 15.464 ml | 30.928 ml |
5 mM | 0.619 ml | 3.093 ml | 6.186 ml |
10 mM | 0.309 ml | 1.546 ml | 3.093 ml |
5 mM | 0.062 ml | 0.309 ml | 0.619 ml |
overview | NS6180 is a highly selective inhibitor of KCa3.1 ion channels with an IC50 value of 9nM, which prevents T cell activation and inflammatory response. |
highly selective inhibitor | 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 inhibitor in 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 rat 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. |
biological activity | NS6180 is a highly selective inhibitor of KCa3.1 ion channel with an IC50 value of 9nM, which prevents T cell activation and inflammatory response. |