ACT-777991 

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^[1].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

550.48

C₂₀H₂₀F₆N₈O₂S

1967811-46-6

OCC[C@@H](N(C(CN1C=NC(C)=N1)=O)CC2)CN2C(SC(C(F)(F)F)=N3)=C3C4=CN=C(C(F)(F)F)N=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Meyer EA, et al. Discovery of Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist for Antigen-Driven and Inflammatory Pathologies. J Med Chem. 2023 Mar 23;66(6):4179-4196.  [Content Brief]