CXCR3 Antagonist

TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a K_i of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC₅₀ and EC₉₀ of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (K_i) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.

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.

NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (¹²⁵I)CXCL10 and (¹²⁵I)CXCL11 specific binding with K_i of 1.5 and 3.2 nM, respectively.

AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.

CXCR3 antagonist 1 (compound 6c) is a selective and non-cytotoxic CXCR3 antagonist (IC₅₀=0.06 µM). CXCR3 antagonist 1 has potential in researching inflammatory diseases (including inflammatory bowel disease, multiple sclerosis, rheumatoid arthritis, and diabetes).

ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC₅₀ value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.

Hypoglaucin A is a CXCR3 antagonist with an IC₅₀ of 0.47 μM. Hypoglaucin A can be used for the research of inflammation.