CAS NO: | 851916-42-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | MK-0812 Succinate is a potent and selectiveCCR2antagonist with high affinity atCCR2. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | MK-0812 is a potent and selective CCR2 antagonist[1]. 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, 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 IC50for MK-0812 in whole blood assays is 8 nM[2] | ||||||||||||||||
体内研究 (In Vivo) | MK-0812 (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, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6Chimonocytes and a corresponding elevation in the CCR2 ligand CCL2[1]. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 587.63 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C28H40F3N3O7 | ||||||||||||||||
CAS 号 | 851916-42-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 32 mg/mL(54.46 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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