C-021 (dihydrochloride)

1784252-84-1

540.57

10 mM in DMSO

Immunology/Inflammation; GPCR/G Protein

C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC₅₀s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [³⁵S]GTPgammaS from binding to the receptor with an IC₅₀ of 18 nM^[1]. In Vitro: 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_int value of 17, 377 mL/h/kg^[1]. In Vivo: 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].