10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Desiccated,Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 .
In Vitro
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 IC 50 of 3.2 nM. This value is similar to the potency observed for the inhibition of 125 I-MCP-1 binding by MK-0812 on isolated monocytes (IC 50 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 IC 50 for MK-0812 in whole blood assays is 8 nMMCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G - Ly6C hi 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 Ly6C hi 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
IC50& Target:CCR2
| Isomeric SMILES | CC(C)[C@@]1(CC[C@H](C1)[NH2+][C@H]2CCOC[C@H]2OC)C(=O)N3CCC4=C(C3)C=C(C=N4)C(F)(F)F.C(CC(=O)[O-])C(=O)O |
|---|---|
| PubChem CID | 60196412 |
| Molecular Weight | 587.63 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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