An arylsulfonamide derivative that acts as a CXCR3 antagonist (IC50 = 192nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100uM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t1/2 = 1h; 10mg/kg p.o.) in vivo and display a medium intrinsic clearance (CIint = 17uL/min/mg) in in vitro mouse liver microsome stability test.
Molecular Formula:C₂₂H₁₆F₂N6O₂S
Solubility:DMSO
Primary Target:CXCR3
Primary Target IC50:192nM
Molar Mass:466.46
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
