MK-0812 Succinate
Modify Date: 2024-01-09 00:22:04
MK-0812 Succinate structure
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Common Name | MK-0812 Succinate | ||
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| CAS Number | 851916-42-2 | Molecular Weight | 587.63 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H40F3N3O7 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of MK-0812 SuccinateMK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 on human monocytes. |
| Name | MK-0812 Succinate |
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| Synonym | More Synonyms |
| Description | MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 on human monocytes. |
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| Related Catalog | |
| Target |
CCR2 |
| 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 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[2] |
| In Vivo | 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[1]. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood[2]. |
| Animal Admin | Mice[1] Female BALB/c mice are used between 8 and 10 weeks of age. SCH563705 or MK-0812 are administered in a 0.4% methylcellulose (MC) solution by 30 mg/kg oral gavage (p.o.). Two hours later, the frequency of CD11b+Ly6G-Ly6Chi monocytes and CD11b+Ly6G+Ly6C+ neutrophils is determined by flow cytometry[1] . |
| References |
| Molecular Formula | C28H40F3N3O7 |
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| Molecular Weight | 587.63 |
| Storage condition | 2-8℃ |
| MK-0812 (Succinate) |