In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Acalabrutinib (ACP-196) 是选择性的第二代BTK抑制剂,抑制B细胞表面原抗体信号通路的激活,IC50为3 nM。它具有很好的靶标特异性,对BTK的选择性比对其他TEC激酶家族成员如ITK、TXK、BMK和TEC的选择性高323-, 94-, 19-, 9-倍。对EGFR没有活性。
MoreU0126 是一种有效,非 ATP 竞争性的,选择性的 MEK1 和 MEK2 抑制剂,IC50 分别为 72 nM 和 58 nM。U0126 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 抑制剂.
MorePyridone 6是一种泛JAK抑制剂,对JAK2, TYK2, JAK3和JAK1的IC50分别为1nM,1nM,5 nM和15 nM
MoreMagnesium sulfate 是一种钙拮抗剂和有效的 L 型钙通道抑制剂,也是一种宫缩抑制剂。Magnesium sulfate 具有抗炎、抗惊厥、血管舒张和神经保护的作用。Magnesium sulfate 可用于先兆子痫/子痫等疾病的研究
MorePtdIns (4)-P1-fluorescein (ammonium salt) is a fluorescent derivative of phosphatidylinositol
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