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.
Atorvastatin calcium, a hydrophilic inhibitor, inhibits the 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Atorvastatin hemicalcium salt 是高活性HMG-CoA还原酶抑制剂,IC50为8 nM。
MoreGo6976 is a potent protein kinase C (PKC) inhibitor (IC50 = 7.9 nM), selectively inhibits PKCα, and PKCβ1 (IC50 values are 2.3 and 6.2 nM respectively).
MoreTacrolimus (FK506)是一种免疫抑制剂和大环内酯类抗生素,用于同种异体的器官移植,可以降低病人的免疫系统的作用。
MoreDexamethasone (DEX), a synthetic glucocorticoid, is widely used in clinical settings for its anti-inflammatory effect. Dexamethasone (DHAP)是一种抗炎剂和免疫抑制剂。
MoreSorafenib (BAY 43-9006), an orally active multi-kinase inhibitor, targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Sorafenib是Raf-1, B-Raf和VEGFR-2等的多重激酶抑制剂,IC50分别为6 nM, 22 nM和90 nM。
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