1010731-97-1

MLN-3897, also known as AVE-9897, is a C-C Motif Chemokine Receptor 1 (CCR1) antagonist potentially for the treatment of multiple sclerosis and rheumatoid arthritis. MLN3897 abrogates its effects by inhibiting Akt signaling. Moreover, MM cell-to-OC adhesion was abrogated by MLN3897, thereby inhibiting MM cell survival and proliferation. MLN3897 demonstrates significant impairment of OC formation (by 40%) and function (by 70%), associated with decreased precursor cell multinucleation and down-regulation of c-fos signaling.

CCR1 antagonist 10 (example 1) 是一种有效的具有口服活性的 CCR1 拮抗剂。CCR1 antagonist 10 抑制 125I-MIP-1α 与 THP-1 细胞膜的结合，Ki 值为 2.3 nM。