CIAC001, a pyruvate kinase PKM2 inhibitor, exhibits anti-neuroinflammatory properties. It effectively suppresses LPS-induced production of proinflammatory nitric oxide (NO) and provides protection to immunologically active BV-2 cells with an IC50 value of 2.5 μM. Additionally, CIAC001 demonstrates anti-neuroinflammation effects in mouse models and attenuates chronic morphine-induced addiction [1].

CIAC001 (10 μM; 6 hours) inhibits LPS-induced (200 ng/mL) morphological changes in microglia in BV-2 cells [1].

CIAC001 administered intraperitoneally at doses of 20 µg/kg and 0.2 mg/kg, once daily for seven days, dose-dependently mitigated naloxone-induced withdrawal jumping in morphine-dependent mice and significantly inhibited the development of behavior sensitization induced by morphine during the induction phase [1]. Additionally, CIAC001 at a dose of 20 mg/kg, given intraperitoneally once daily for seven days, did not notably impair memory or cognitive function in the Y maze test in mice [1].