CXCR3 Antagonist

An arylsulfonamide derivative that acts as a CXCR3 antagonist (IC₅₀ = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t_1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CI_int = 17 µL/min/mg) in in vitro mouse liver microsome stability test.

An arylsulfonamide derivative that acts as a CXCR3 antagonist (IC₅₀ = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t_1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CI_int = 17 µL/min/mg) in in vitro mouse liver microsome stability test.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Cell permeable: yes

Primary Target
CXCR3

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).

Crosignani, S., et al. 2010. Bioorg. Med. Chem. Lett.20, 3614.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany