J-113863 是选择性的CCR1 (CD18)拮抗剂，有抗炎作用，对人和小鼠CCR1受体的IC50值分别为 0.9 和 5.8 nM。它是人CCR3的强效拮抗剂，还是小鼠CCR3的弱效拮抗剂，IC50分别为 0.58 和 460 nM。

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

The chemotaxis of the following cells were inhibited by J-113863. Modified Vaccinia virus Ankara (MVA) but not MVA and vaccinia virus (VACV) infected MH-S cells increase the expression of the CXCR2 acting chemokine CXCL2. MH-S cells constitutively produce CCL2 and CCR1 acting chemokines CCL3, CCL5 and CCL9. Consequently, supernatants of mock treated and virus infected MH-S cells induce chemotaxis of murine promyelocyte MPRO cells and human monocytic THP-1 cells at the same level. However, supernatants of MVA infected MH-S cells significantly increase chemotaxis of the CCR2 deficient human monocytic cell line U-937.

J-113863 treatment improves paw inflammation and joint damage, and dramatically decreases cell infiltration into joints in arthritic mice.

353791-85-2

C30H37Cl2IN2O2

655.44

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years