mk-0812

MK-0812 is a potent and selective small molecule antagonist of the C-C chemokine receptor type 2 (CCR2). It was developed by Merck for the treatment of inflammatory and autoimmune diseases. MK-0812 binds CCR2 with low nanomolar affinity (IC50 ~5 nM) and inhibits CCL2-mediated chemotaxis. It has been evaluated in clinical trials for relapsing-remitting multiple sclerosis and rheumatoid arthritis but did not demonstrate sufficient efficacy in these indications. Preclinical studies have also explored its potential in cancer metastasis models, where it reduced monocytic myeloid-derived suppressor cells and lung metastases in humanized mice[1][3][4][6][8][9].

Other names

624733-88-6CHEMBL3305901CHEMBL-3305901CHEMBL 3305901