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Nenocorilant
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nenocorilant图片
CAS NO:1496509-78-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
Relacorilant
CORT125134
产品介绍
Nenocorilant (Relacorilant) 是一种口服有效的糖皮质激素受体 (GR) 拮抗剂,Ki值为 0.15 nM。Nenocorilant 具有促凋亡 (pro-apoptotic) 作用,并与细胞毒性药物联合使用提高药效。Nenocorilant 可用于肿瘤研究。
生物活性

Nenocorilant (Relacorilant) is a potent, orally activityglucocorticoid receptor(GR)antagonist with Kivalue of 0.15 nM. Nenocorilant haspro-apoptoticeffects and improves potency combined with cytotoxic agent. Nenocorilant can be used forcancerresearch[1][2][3].

IC50& Target

Ki: 0.15 nM (glucocorticoid receptor)[1]

体外研究
(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 genesSGK1andMKP1[2].

体内研究
(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.
Clinical Trial
分子量

587.55

Formula

C26H21F4N7O3S

CAS 号

1496509-78-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.