LC10

一种胆汁酸类脂质衍生物（来源于胆汁酸胆烷酸，pKa=6.38），已用于制备自组装且可穿透皮肤的脂质纳米粒（LNPs）。LC10脂质纳米粒在100nM浓度下可抑制人正常角质形成细胞（NHEKs）的增殖，并在50、100和200nM浓度下降低人外周血单个核细胞（PBMCs）中TNF-α、IL-17和IL-23的水平。此外，LC10脂质纳米粒在银屑病小鼠模型中，以10mg/kg的剂量局部给药，可减少咪喹莫特诱导的银屑病样皮损和体重减轻。A lipidoid derivative of lithocholic acid; has been used in the generation of self-assembling skin-permeable LNPs; LC10 LNPs inhibit the proliferation of NHEKs at 100 nM and reduce TNF-α, IL-17, and IL-23 levels in human PBMCs at 50, 100, and 200 nM; LC10 LNPs reduce imiquimod-induced psoriatic-like plaques and weight loss at 10 mg/kg topically in a mouse model of psoriasis.分子式C46H86N2O2 • HCl分子量735.7C[C@H](CCC(NCCN(CCCCCCCCCC)CCCCCCCCCC)=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C