ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11.
ACT-777991 inhibits hEGR with an IC50 value of 26 μM in CHO cells[1].
ACT-777991 (1 μM; 45 min) is stable in microsomes and hepatocytes across humans, rats, and dogs[1].
ACT-777991 (0.01-1 μM; ) inhibits the migration of both human and mouse-activated T cells toward CXCL11 with IC50s range of 3.2-64 nM and 4.9-21 nM, respectively[1].
ACT-777991 (1 nM, 5 nM, 20 nM, and 50 nM) inhibits CXCR3-mediated chemotaxis of human and mouse T cells[1].
ACT-777991 (0.5 mg/kg, 1 mg/kg; i.v.; single dose) has low in vivo plasma clearance in male Wistar rats (14/156) or Beagle dogs (5/15)[1].
ACT-777991 (0.006-2 mg/g food; po; started 3 days before and 72 h post LPS challenge) dose-dependently inhibits chemotaxis of CXCR3+ T cells in vivo in mouse model[1].