ml 221

ML221 is a potent apelin /APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

Anticanceragent 221 (Compound 4h) is an orally active anticancer and antioxidant agent. It exhibits cytotoxicity against cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL) and induces apoptosis. It demonstrates antioxidant activity with an IC50 of 42.46 μM in the DPPH assay. In mouse models, Anticanceragent 221 shows antitumor efficacy against breast cancer.

ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson's disease (PD) rats.