NS-6180
中文名称 | NS-6180 |
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中文同义词 | 4-[[3-(三氟甲基)苯基]甲基]-2H-1,4-苯并噻嗪-3(4H)-酮;化合物NS6180;化合物MERICITABINE;NS 6180,KCA3.1(IK)通道阻止器 |
英文名称 | NS-6180 |
英文同义词 | 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号 | 353262-04-1 |
分子式 | C16H12F3NOS |
分子量 | 323.33 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;Inhibitors |
Mol文件 | 353262-04-1.mol |
结构式 |
NS-6180 性质
沸点 | 476.9±45.0 °C(Predicted) |
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密度 | 1.375±0.06 g/cm3(Predicted) |
储存条件 | Sealed in dry,2-8°C |
溶解度 | 在DMSO中的溶解度为20mg/mL,澄清 |
酸度系数(pKa) | 0.53±0.20(Predicted) |
形态 | 粉末 |
颜色 | 白色至米色 |
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 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.
NS6180是KCa3.1离子通道高效选择性抑制剂,IC50值9nM,阻止T细胞活化和炎症反应。更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-15707 | NS-6180 NS6180 | 353262-04-1 | 5mg | 650元 |
2024/08/19 | HY-15707 | NS-6180 NS6180 | 353262-04-1 | 10mM * 1mLin DMSO | 715元 |