XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo. XVA143 is an antagonist of both mouse and human CR3, inhibits the ability of P. gingivalis to persist in the mouse host and cause periodontal bone loss.

XVA143 (1 μM) completely abolishes binding of ICAM-1 to LFA-1 in Mn 2+ and Mg 2+ /EGTA, with no hint of agonism[1]. XVA143 restores rolling of the α L -E310A β 2 mutant by inducing extension of α L[2]. Cell Viability Assay[1]Cell Line: K562 cells. Concentration: 0, 0.2, 0.5 and 1 μM. Incubation Time: Result: Potent against the weakest activator (2 mM Mg 2+ /1 mM EGTA, IC 50 ~10 -3 nM) and least potent against the strongest activator (1 mM Mn 2+ , IC 50 ~10 -3 nM). Cell Viability Assay[1]Cell Line: Wild-type murine lymphocytes[1]. Concentration: 100 μM. Incubation Time: Result: Induced a 50% increase in rolling fraction compared to vehicle-treated control cells ((from 27±5% to 41±7%).

264275-77-6

C25H21Cl2N3O8

562.36

XVA143;XVA143

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years