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编 号:F480307
分子式:C28H40F3N3O7
分子量:587.63
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.

体内研究:
MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood.

体外研究:
MK-0812 is a potent and selective CCR2 antagonist. MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50 of 3.2 nM. This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50 4.5 nM). In fact, MK-0812 not only completely blocks the shape change response to exogenous MCP-1, but also results in a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM
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