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MK-0812 Succinate - 10mM in DMSO, high purity , CAS No.851916-42-2(DMSO)

  • 10mM in DMSO
Item Number
M655252
Grouped product items
SKUSizeAvailabilityPrice Qty
M655252-1ml
1ml
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$233.90

Basic Description

Specifications & Purity10mM in DMSO
Storage TempDesiccated,Store at -80°C
Shipped InIce chest + Ice pads
Product Description

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

Names and Identifiers

Canonical SMILES O=C([C@]1(C(C)C)C[C@H](N[C@H]2CCOC[C@H]2OC)CC1)N3CCC(N=CC(C(F)(F)F)=C4)=C4C3.O=C(O)CCC(O)=O
Molecular Weight 587.63

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