MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2 .In VitroMK-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 VivoMK-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.Form:SolidIC50& Target:CCR2. Specification: 0.99 Molecular Formula: C28H40F3N3O7 Molecular Weight: 587.63 PubChem CID: 60196412 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
- UPC:
- 51172333
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- M648000-5mg
- CAS:
- 851916-42-2
- Product Size:
- 5mg
