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Nenocorilant

Names

[ CAS No. ]:
1496509-78-4

[ Name ]:
Nenocorilant

Biological Activity

[Description]:

Nenocorilant (Relacorilant) is a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent. Nenocorilant can be used for cancer research[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Apoptosis >> Caspase
Signaling Pathways >> GPCR/G Protein >> Glucocorticoid Receptor

[Target]

Ki: 0.15 nM (glucocorticoid receptor)[1]


[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[1]. Nenocorilant (Relacorilant) (100 nM; 4 h; MIA PaCa-2 and OVCAR5 cells) prevents dex-mediated upregulation of both GR target genes SGK1 and MKP1[2].

[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[1]. Animal Model: Female Balb/c nude mice[1] 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.

[References]

[1]. Greenstein AE, et, al. Glucocorticoid receptor antagonism promotes apoptosis in solid tumor cells. Oncotarget. 2021 Jun 22;12(13):1243-1255.

[2]. Stringer-Reasor EM, et, al. Glucocorticoid receptor activation inhibits chemotherapy-induced cell death in high-grade serous ovarian carcinoma. Gynecol Oncol. 2015 Sep;138(3):656-62.

[3]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical

Chemical & Physical Properties

[ Molecular Formula ]:
C26H21F4N7O3S

[ Molecular Weight ]:
587.55

Related Compounds