MK-0812 succinate

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 is a potent and selective CCR2 antagonist. 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.

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. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood.

MK 0812 Succinate | MK0812 Succinate

GPCR/G Protein

Chemokine Receptor

Chemokine Receptor

Inflammation/Immunology

Multiple Sclerosis

851916-42-2

587.6283

C28H40F3N3O7

>98% (HPLC)

DMSO: ≥ 32 mg/mL

O=C([C@@]1(C(C)C)C[C@@H](N[C@@H]2[C@H](OC)COCC2)CC1)N3CC4=C(N=CC(C(F)(F)F)=C4)CC3.O=C(O)CCC(O)=O

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-, butanedioate (1:1)

(-20℃)

With Ice Pack

≥ 2 years