ITX5061

ITX5061 is an orally active type II non-competitive p38 MAPK inhibitor. ITX5061 increases HDL-C levels by inhibiting SR-BI activity. ITX5061 also moderately elevates ApoA-I levels. ITX5061 reduces early atherosclerotic lesions in the aortic arch of mice fed an atherogenic diet. ITX5061 can be used in the research of atherosclerosis^[1]. IC50 & Target:p38 MAPK, SR-B1^[1] In Vitro:ITX5061 (1 μM) significantly inhibits SR-BI-mediated HDL uptake in HEK 293 cells overexpressing SR-BI^[1]. In Vivo:ITX5061 (30 mg/kg; daily; 7 days) increases HDL-C and apoA-I levels, shifts HDL to larger particles, and reduces HDL-CE catabolism and hepatic uptake in HuAITg mice, with a 50% increase in HDL-C and 15% increase in apoA-I after one week of treatment^[1].
ITX5061 (30 mg/kg; daily; 7 days) increases HDL-C levels in WT mice in an SR-BI-dependent manner, with no effect on HDL-C in SR-BI^−/− mice^[1].
ITX5061 (0.037% incorporated into diet; daily; 18 weeks) increases HDL-C by 30% and reduces early atherosclerotic lesions in the aortic arch by 40% in Ldlr⁺/⁻ mice fed a Paigen diet for 18 weeks, regardless of CETP expression^[1].