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| | NS-6180 Basic information |
| Product Name: | NS-6180 | | Synonyms: | NS 6180;NS6180;NS-6180;4-[[3-(Trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one;NS6180;NS-6180;NS 6180;CS-1648;2H-1,4-Benzothiazin-3(4H)-one, 4-[[3-(trifluoromethyl)phenyl]methyl]-;NS6180 >=98% (HPLC) | | CAS: | 353262-04-1 | | MF: | C16H12F3NOS | | MW: | 323.33 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 353262-04-1.mol |  |
| | NS-6180 Chemical Properties |
| 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 | | pka | 0.53±0.20(Predicted) | | form | powder | | color | white to beige |
| Hazard Codes | Xi,N | | Risk Statements | 43-51/53 | | Safety Statements | 61 | | RIDADR | UN 3077 9 / PGIII | | WGK Germany | 3 |
| | NS-6180 Usage And Synthesis |
| 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. | | 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. |
| | NS-6180 Preparation Products And Raw materials |
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