| Description | CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes. |
| In vivo | CCR2 antagonist 5 (compound 8d) has good CV safety profile. It does not induce dose-dependent or notable effects on most cardiohemodynamic, functional respiratory, and electrophysiological parameters up to 10 mg/kg (i.v.) with plasma level at 70 µM in an anesthetized dog.[1] CCR2 antagonist 5 dose-dependently inhibits the influx of leukocytes, monocytes/macrophages, and T-lymphocytes into the peritoneal cavity with an ED50 of 3 mg/kg p.o. bid in a thioglycollate-induced peritonitis (TG) model.[1]CCR2 antagonist 5 has amendable oral bioavailability in dogs and primates.[1] |
| Target activity | CCR2 (mouse):9.6 μM (Ki), CCR2 (human):37 nM (IC50) |
| Synonyms | JNJ-41443532, JNJ-41443532 Free Base, JNJ 41443532, JNJ41443532 |
| molecular weight | 482.52 |
| Molecular formula | C22H25F3N4O3S |
| CAS | 1228650-83-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (103.62 mM) |
| References | 1. Di Prospero NA, Artis E, Andrade-Gordon P, Johnson DL, Vaccaro N, Xi L, Rothenberg P. CCR2 antagonism in patients with type 2 diabetes mellitus: a randomized, placebo-controlled study. Diabetes Obes Metab. 2014 Nov;16(11):1055-64. doi: 10.1111/dom.12309. Epub 2014 May 25. PubMed PMID: 24798870. |