| Description | MLN-3897 (CCR1 antagonist 10) is an orally active antagonist of CCR1 with a Ki of 2.3 nM for 125I-MIP-1α binding to THP-1 cell membranes. MLN-3897 inhibits Akt signaling and MM cell survival and proliferation. |
| Synonyms | AVE9897, AVE 9897, CCR1 antagonist 10, AVE-9897 |
| molecular weight | 519.03 |
| Molecular formula | C30H31ClN2O4 |
| CAS | 1010731-97-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Pusalkar S, et al. Metabolism, Excretion and Pharmacokinetics of MLN3897, a CCR1 Antagonist, in Humans. Drug Metab Lett. 2016;10(1):22-37. 2. Vergunst CE, et al. MLN3897 plus methotrexate in patients with rheumatoid arthritis: safety, efficacy, pharmacokinetics, and pharmacodynamics of an oral CCR1 antagonist in a phase IIa, double-blind, placebo-controlled, randomized, proof-of-concept study. Arthritis Rheum. 2009 Dec;60(12):3572-81. 3. Lu C, et al. Quantitative prediction and clinical observation of a CYP3A inhibitor-based drug-drug interactions with MLN3897, a potent C-C chemokine receptor-1 antagonist. J Pharmacol Exp Ther. 2010 Feb;332(2):562-8. 4. Vallet S, et al. MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts. Blood. 2007 Nov 15;110(10):3744-52. 5. Kenneth G. Carson, et al. Ccr1 antagonists for the treatment of i.a. demyelinating inflammatory disease. WO2004043965A1. |