Nenocorilant

Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with K i value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research In Vitro Nenocorilant (Relacorilant) (0-1000 nM; 0-72 h; OvCa cells) has pro-apoptotic effects and reverses the effects of cortisol and partially restored Paclitaxel and Gemcitabine induction of tumor-cell apoptosis. Nenocorilant (Relacorilant) (100 nM; 4 h; MIA PaCa-2 and OVCAR5 cells) prevents dex-mediated upregulation of both GR target genes SGK1 and MKP1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Nenocorilant (Relacorilant) (30 mg/kg; p.o.; once every four days, for 25 d; female Balb/c nude mice) improves the efficacy and promotes apoptotic activity of cytotoxic therapy in xenograft models under physiological cortisol conditions . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Balb/c nude mice Dosage: 30 mg/kg Administration: Oral administration; once every four days, for 25 days Result: Inhibited tumor growth and increased the expression level of caspase 3. IC50& Target:Ki: 0.15 nM (glucocorticoid receptor)

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