Relacorilant (CORT 125134)是一种有效的糖皮质激素受体（GR）拮抗剂。
Cas No.:1496510-51-0
Sample solution is provided at 25 µL, 10mM.
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Relacorilant (CORT 125134) is a potent and selective glucocorticoid receptor (GR) antagonist[1-2]. Relacorilant can increase the abundance and function of NK and other immune cells in the tumor microenvironment, while promoting immune responses in malignancies characterized by excessive glucocorticoid production (GC+). Relacorilant is used in research related to Cushing's syndrome (CS) and tumors, such as adrenocortical carcinoma and platinum-resistant ovarian cancer[3-4].
In vitro, Relacorilant (300nM) was co-administered with paclitaxel to OVCAR5 ovarian cancer cells. Relacorilant restored the potency (IC50) of paclitaxel, and enhanced the activity of various cytotoxic agents, including paclitaxel, carboplatin, and gemcitabine[5]. Relacorilant (1-10µM) was co-administered with docetaxel to docetaxel-resistant PC3-DR prostate cancer cells. Relacorilant significantly reduced the IC50 of docetaxel in a concentration-dependent manner and enhanced docetaxel-induced apoptosis[6].
In vivo, in an aged female mouse skin experiment, Relacorilant (60mg/kg/day) was administered to 18-month-old C57BL/6J female mice via oral chow for 8 weeks. Relacorilant significantly inhibited the gene expression of Scnn1g in the skin[7]. Relacorilant (60mg/kg/day) was administered to 8-week-old C57BL/6J male mice via gavage for 5 days. Relacorilant improved sustained corticosterone exposure-induced hyperinsulinemia and immunosuppression (e.g., reductions in leukocytes and lymphocytes) and exhibited antagonistic effects on glucocorticoid receptor (GR) target gene expression in peripheral tissues (liver, adrenal glands, pituitary)[8].
References:
[1] Greenstein AE, Habra MA, Wadekar SA, et al. Adrenal tumors provide insight into the role of cortisol in NK cell activity. Endocr Relat Cancer. 2021 Jun 29;28(8):583-592.
[2] Dua VK, Verma G, Singh B, et al. Anti-malarial property of steroidal alkaloid conessine isolated from the bark of Holarrhena antidysenterica. Malar J. 2013 Jun 10;12:194.
[3] Colombo N, Van Gorp T, Matulonis UA, et al. Relacorilant + Nab-Paclitaxel in Patients With Recurrent, Platinum-Resistant Ovarian Cancer: A Three-Arm, Randomized, Controlled, Open-Label Phase II Study. J Clin Oncol. 2023 Oct 20;41(30):4779-4789.
[4] Pivonello R, Bancos I, Feelders RA, et al. Relacorilant, a Selective Glucocorticoid Receptor Modulator, Induces Clinical Improvements in Patients With Cushing Syndrome: Results From A Prospective, Open-Label Phase 2 Study. Front Endocrinol (Lausanne). 2021 Jul 14;12:66286.
[5] Greenstein AE, Hunt HJ. Glucocorticoid receptor antagonism promotes apoptosis in solid tumor cells. Oncotarget. 2021 Jun 22;12(13):1243-1255.
[6] Sanchez-Hernandez ES, Ochoa PT, Suzuki T, et al. Glucocorticoid Receptor Regulates and Interacts with LEDGF/p75 to Promote Docetaxel Resistance in Prostate Cancer Cells. Cells. 2023 Aug 11;12(16):2046.
[7] Ali A, Fossas De Mello N, et al. The Effect of Glucocorticoid and Mineralocorticoid Receptor Antagonists in the Skin of Aged Female Mice. Int J Mol Sci. 2025 Aug 28;26(17):8346.
[8] Viho EMG, Kroon J, Feelders RA, et al. Peripheral glucocorticoid receptor antagonism by relacorilant with modest HPA axis disinhibition. J Endocrinol. 2022 Dec 22;256(2):e220263.
Relacorilant (CORT 125134)是一种有效的糖皮质激素受体（GR）拮抗剂[1-2]。Relacorilant可以增加肿瘤微环境中NK和其他免疫细胞的丰度和功能，同时能促进具有糖皮质激素过量产生（GC+）情况的恶性肿瘤中的免疫反应。Relacorilant可用于库欣综合征（CS）和肿瘤（如肾上腺皮质癌、铂耐药卵巢癌）的相关研究[3-4]。
在体外，Relacorilant（300nM）与紫杉醇联合处理OVCAR5卵巢癌细胞，Relacorilant可恢复紫杉醇的效力（IC50），并能改善紫杉醇、卡铂、吉西他滨等多种细胞毒性药物的活性[5]。Relacorilant（1-10μM）与多西他赛联合处理对多西他赛耐药的PC3-DR前列腺癌细胞，Relacorilant以浓度依赖的方式显著降低PC3-DR对多西他赛的IC50值，并增强多西他赛诱导的细胞凋亡[6]。
在体内，在老龄雌性小鼠皮肤实验中，Relacorilant（60mg/kg/day）通过口服饲料给药处理18月龄C57BL/6J雌性小鼠8周，Relacorilant显著抑制了皮肤中Scnn1g的基因表达[7]。Relacorilant（60mg/kg/天）通过灌胃给药处理8周龄C57BL/6J雄性小鼠5天，Relacorilant可改善由持续皮质酮暴露诱导的高胰岛素血症和免疫抑制（如白细胞、淋巴细胞减少），可抑制外周组织（肝脏、肾上腺、垂体）中的糖皮质激素受体（GR）靶基因表达表现出拮抗作用[8]。
| Cell experiment [1]: | |
Cell lines | MIA PaCa-2 cells (human pancreatic carcinoma cell line) and OVCAR5 cells (human ovarian carcinoma cell line) |
Preparation Method | Cells were grown in media supplemented with 2.5% fetal bovine serum (FBS) or 2.5% charcoal-dextran stripped FBS. For kinetic apoptosis assays, MIA PaCa-2 cells were seeded with a nuclear dye and a fluorescent caspase 3/7 substrate. For viability assays, OVCAR5 and other cell lines were seeded in 96-well plates. In the presence of physiological Cortisol (400nM) or the GR agonist dexamethasone (100nM), cells were treated with Relacorilant (300nM) and various cytotoxic agents (e.g., Paclitaxel, Carboplatin, Gemcitabine) for 3 days (viability) or monitored kinetically (apoptosis). |
Reaction Conditions | 300nM; 3 days. |
Applications | In MIA PaCa-2 cells, Cortisol (400nM) significantly reduced paclitaxel-induced apoptosis, and Relacorilant reversed this effect, partially restoring apoptosis. In OVCAR5 cells, dexamethasone diminished the potency (increased IC50) and maximal efficacy (increased residual viability) of cytotoxic agents like Carboplatin, Oxaliplatin, Paclitaxel, and Gemcitabine. Relacorilant restored the potency and efficacy of these agents, showing a dose-dependent effect. A screen of 19 cytotoxic agents indicated that Relacorilant most consistently improved the activity of microtubule-targeting agents. |
| Animal experiment [2]: | |
Animal models | C57BL/6J female mice |
Preparation Method | Mice were randomly assigned and fed a control diet or a chow containing the selective glucocorticoid receptor antagonist, Relacorilant (60mg/kg/day), for eight weeks. Body mass and food consumption were monitored throughout. At the end of the study, all mice were euthanized, and dorsal skin tissues were collected for analysis. |
Dosage form | 60mg/kg/day; oral; 8 weeks. |
Applications | Relacorilant treatment significantly decreased the mRNA expression of Scnn1g, a subunit of the epithelial sodium channel, in the skin. The treatment did not significantly alter the epidermal thickness, the expression of keratinocyte proliferation markers, the expression of key inflammatory cytokines, or the expression of regulators of glucocorticoid activity. |
References: | |
| Cas No. | 1496510-51-0 | SDF | |
| Canonical SMILES | O=C(C1=CC(C(F)(F)F)=CC=N1)[C@@]2(CN(S(=O)(C3=CN(C)N=C3)=O)CC4)C4=CC5=C(C=NN5C6=CC=C(F)C=C6)C2 | ||
| 分子式 | C27H22F4N6O3S | 分子量 | 586.56 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7049 mL | 8.5243 mL | 17.0486 mL |
| 5 mM | 341 μL | 1.7049 mL | 3.4097 mL |
| 10 mM | 170.5 μL | 852.4 μL | 1.7049 mL |
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