CCR2 antagonist 5_product_DataBase

Bioactivity	CCR2 antagonist 5 is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). CCR2 antagonist 5 displays a Ki of 9.6 µM for mCCR2 binding. CCR2 antagonist 5 can be used in the research of inflammatory disease[1].
In Vivo	CCR2 antagonist 5 (compound 8d) 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 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 has amendable oral bioavailability in dogs and primates. Pharmacokinetic parameters (p.o.)[1]: Species
Name	CCR2 antagonist 5
CAS	1228650-83-6
Formula	C22H25F3N4O3S
Molar Mass	482.52
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Zhang X, et al. Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate. ACS Med Chem Lett. 2012 Oct 8;3(12):1039-44.

PeptideDB