MK-0812

Research use only, not for human use.

A potent CCR2 specific antagonist that blocks MCP-1 mediated response with an IC50 of 3.2 nM.

A potent CCR2 specific antagonist that blocks MCP-1 mediated response with an IC50 of 3.2 nM; inhibits 125I-MCP-1 binding on isolated monocytes with IC50 of 4.5 nM; reduces macrophage accumulation in adipose tissue in ob/ob mice.Multiple Sclerosis Phase 2 Discontinued.

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, the antagonist 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 MK0812 is a potent and selective small molecule CCR2 antagonist.

MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood. Administration of MK0812 at 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, MK0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2.

MK 0812 | MK0812

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Inflammation/Immunology

Multiple Sclerosis

624733-88-6

469.5403

C24H34F3N3O3

>98% (HPLC)

10 mM in DMSO

CC(C)[C@@]1(CC[C@H](C1)N[C@H]2CCOC[C@H]2OC)C(=O)N3CCC4=NC=C(C=C4C3)C(F)(F)F

D-erythro-Pentitol, 1,5-anhydro-2,3-dideoxy-3-[[(1R,3S)-3-[[7,8-dihydro-3-(trifluoromethyl)-1,6-naphthyridin-6(5H)-yl]carbonyl]-3-(1-methylethyl)cyclopentyl]amino]-4-O-methyl-

(-20℃)

With Ice Pack

≥ 2 years