CAS NO: | 624733-88-6 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | MK-0812 is a potent and selectiveCCR2antagonist with low nM affinity forCCR2. | ||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50of 3.2 nM. This value is similar to the potency observed for the inhibition of125I-MCP-1 binding by MK-0812 on isolated monocytes (IC504.5 nM). In fact, the antagonist 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 IC50for MK-0812 in whole blood assays is 8 nM[1]MK0812 is a potent and selective small molecule CCR2 antagonist[2]. | ||||||||||||
体内研究 (In Vivo) | MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[1]. Administration of MK0812 at 30 mg/kg, p.o. reduces the frequency of Ly6G-Ly6Chimonocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+neutrophil frequency is observed. In addition, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chimonocytes and a corresponding elevation in the CCR2 ligand CCL2[2]. | ||||||||||||
Clinical Trial | |||||||||||||
分子量 | 469.54 | ||||||||||||
性状 | Solid | ||||||||||||
Formula | C24H34F3N3O3 | ||||||||||||
CAS 号 | 624733-88-6 | ||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||
储存方式 |
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