C-021 dihydrochloride is a potentCC chemokine receptor-4 (CCR4)antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse withIC₅₀s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [³⁵S]GTPγS from binding to the receptor with anIC₅₀of 18 nM^[1].

The in vitro oxidative metabolic stability of C-021 (Compound 1b) is evaluated by measuring the rate of drug consumption in human liver microsomes (HML), thus providing intrinsic clearance values (CLint). C-021 exhibits CL_intvalue of 17,377 mL/h/kg^[1].

The potency of C-021 (Compound 1b) is evident after subcutaneous administration in the murine oxazolone-induced contact hypersensitivity test, a known model of acute skin inflammation. When C-021 is administered orally, however, very little inhibition is observed^[1].
C-021 (1 mg/kg; i.p.; daily; for 3 days) significantly less microgliosis in acute liver failuremice^[2].

540.57

Solid

C₂₇H₄₃Cl₂N₅O₂

1784252-84-1

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)