化合物MK-0812 Succinate T16091

Product Introduction
Bioactivity


英文名: MK-0812 Succinate

描述: MK-0812 Succinate 是一种选择性CCR2拮抗剂。

体外活性: MK-0812 not only fully blocks the shape change response to exogenous MCP-1 but also causes 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. MK-0812 fully blocks all MCP-1 mediated response in a concentration-dependent manner (IC50: 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) [2].

体内活性: MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in the blood. MK-0812 treatment induces a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2. MK-0812 (30 mg/kg, p.o.) decreases the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed [1][2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 28 mg/mL (47.65 mM)


关键字: MK-0812 Succinate | CC chemokine receptor | MK 0812 | Inhibitor | MK0812 Succinate | MK 0812 Succinate | CCR | MK0812 | MK-0812 | inhibit

相关产品: Eburicoic acid | CCR6 inhibitor 1 | MK-0812 | RS102895 | ZK 756326 | 5-Hydroxy-7,8-dimethoxyflavanone | SB-649701 | PF-04634817 | CCR2-RA-[R] | CCR2 antagonist 5

相关库: ReFRAME Related Library | Cytokine Inhibitor Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Chemokine Inhibitor Library

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