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|---|---|---|---|---|---|---|---|
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| 描述 | Cintirorgon, also known as LYC-55716, is a first-in-class selective oral bioactive RORγ agonist. Cintirorgon modulates gene expression in RORγ-expressing T-lymphocyte immune cells, resulting in enhanced effector function, decreased immunosuppression, reduced tumour growth, and improved survival[1][2]. |
| Administration | Dosage | Frequency | Description | References | ||
| C57BL/6 mice | Lewis lung carcinoma (LLC) model | Intraperitoneal injection | 50 mg/kg | Once daily for two weeks | Evaluate the antitumor efficacy of LYC-55716 in the LLC model. | J Exp Clin Cancer Res. 2022 Apr 23;41(1):155 |
| Sprague Dawley rats | Cecal ligation and puncture (CLP)-induced sepsis model | Intraperitoneal injection | 150 mg/kg | Once daily for 7 days | To investigate the effect of LYC-55716 on intestinal immune function in septic rats. | Heliyon. 2023 Jun 28;9(7):e17766 |
| Wistar rats | 14-day-old neonatal rat infection model | Oral | 10 mg/kg body weight | Once every two days, continued until 72 hours post-infection | To evaluate the protective effect of Cintirorgon on S. Typhimurium-infected neonatal rats, results showed that Cintirorgon significantly improved survival rates, alleviated weight loss and diarrhea symptoms, and reduced intestinal bacterial load. | Emerg Microbes Infect. 2024 Dec;13(1):2417867 |
| Animal study | Upon oral administration, Cintirorgon selectively binds to the nuclear receptor transcription factor RORγ, forming a receptor complex that translocates to the nucleus and binds to ROREs to enhance the function, proliferation and survival of Th17 and Tc17 cells. RORγ is a nuclear receptor transcription factor involved in the differentiation of Th17/Tc17 and plays a key role in immune activation[1]. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03396497 | Non-small Cell Lung Cancer | Phase 1 | Recruiting | March 2019 | United States, Colorado ... 展开 >> Lycera Investigational Site Recruiting Aurora, Colorado, United States, 80045 United States, Michigan Lycera Investigational Site Recruiting Ann Arbor, Michigan, United States, 48109 United States, Tennessee Lycera Investigational Site Recruiting Nashville, Tennessee, United States, 37203 United States, Washington Lycera Investigational Site Recruiting Seattle, Washington, United States, 98109 收起 << |
| NCT02929862 | Cancer | Phase 1 Phase 2 | Recruiting | March 2019 | - |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.66mL 0.33mL 0.17mL |
8.28mL 1.66mL 0.83mL |
16.57mL 3.31mL 1.66mL |
|
| CAS号 | 2055536-64-4 |
| 分子式 | C27H23F6NO6S |
| 分子量 | 603.53 |
| SMILES Code | FC(F)OC1=CC(F)=CC(C2=CC3=C(O[C@@H](CC(C)(C(O)=O)C)CN3S(C4=CC(C(F)(F)F)=CC=C4)(=O)=O)C=C2)=C1 |
| MDL No. | MFCD31544352 |
| 别名 | Lyc-55716 |
| 运输 | 蓝冰 |
| InChI Key | GULSIMHVQYBADX-FQEVSTJZSA-N |
| Pubchem ID | 124126348 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 110 mg/mL(182.26 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 无水乙醇: 100 mg/mL(165.69 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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