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C 101248是一种选择性且强效的小鼠和人类串联孔道卤素抑制K+通道1(THIK-1, IC50= 50 nM)抑制剂,对K2P家族成员TREK-1和TWIK-2以及Kv2.1无活性。C 101248能够阻断小鼠海马微胶质细胞中THIK-1 K+电流的整细胞膜片钳记录中的音调和ATP激发的电流。C 101248通过防止NLRP3依赖性IL-1β的释放,从而减少在分离的微胶质细胞中的神经炎症。
C 101248是一种选择性且强效的小鼠和人类串联孔道卤素抑制K+通道1(THIK-1, IC50= 50 nM)抑制剂,对K2P家族成员TREK-1和TWIK-2以及Kv2.1无活性。C 101248能够阻断小鼠海马微胶质细胞中THIK-1 K+电流的整细胞膜片钳记录中的音调和ATP激发的电流。C 101248通过防止NLRP3依赖性IL-1β的释放,从而减少在分离的微胶质细胞中的神经炎症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | ¥ 2,430 | 现货 | |
50 mg | ¥ 9,870 | 现货 |
产品描述 | C 101248 is a selective and potent inhibitor targeting both mouse and human tandem pore domain halothane-inhibited K+ channel 1 (THIK-1, IC50= 50 nM), without affecting the K2P family members (TREK-1, TWIK-2) and Kv2.1. This compound effectively blocks tonic and ATP-evoked THIK-1 K+ currents as observed in whole-cell patch-clamp recordings of mouse hippocampal microglia. Additionally, C 101248 mitigates neuroinflammation by inhibiting the NLRP3-dependent release of IL-1β in isolated microglia. |
分子量 | 292.30 |
分子式 | C15H12N6O |
CAS No. | 361368-24-3 |
Smiles | NC1=NON=C1C2=NC3=CC=CC=C3N2CC4=CC=NC=C4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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