产品描述:
Acitretin is a retinoid and an active metabolite of the retinoid etretinate (Item No. 19878) that has antiproliferative activities.{46411,46412} It binds to cellular retinoic acid binding protein I (CRABP-I) and CRABP-II (Kds = 3 and 15 nM, respectively, for the mouse recombinant proteins) but has low affinity for human recombinant retinoic acid receptor-retinoid X receptor (RAR-RXR) heterocomplexes.{46413,46414} Acitretin inhibits proliferation (IC50 = 6.6 µM) and suppresses TNF-α- and IFN-γ-induced protein levels of STAT1, NF-ĸB, and RANTES in HaCaT keratinocytes when used at concentrations up to 50 µM.{46415} It inhibits proliferation of HL-60, SCC4, SCC15, and A431, but not MCF-7, cancer cells, when used at a concentration of 30 µM.{46412} Acitretin (20 µg per mouse) decreases the severity of psoriatic-like skin lesions in K14-VEGF transgenic mice.{46411} Formulations containing acitretin have been used in the treatment of psoriasis.