产品说明书
AC-186
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同义名 : | - |
| CAS号 : | 1421854-16-1 | |
| 货号 : | A958678 | |
| 分子式 : | C18H17F3O | |
| 纯度 : | 99%+ | |
| 分子量 : | 306.322 | |
| MDL号 : | MFCD28502295 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(342.78 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The estrogen-related receptors (ERRs) comprise a small group of orphan nuclear receptor transcription factors. The ERRα and ERRγ isoforms play a central role in the regulation of metabolic genes and cellular energy metabolism. ERRβ is the important in the maintenance of embryonic stem cell pluripotency[1]. The selective ERβ agonist AC-186 was evaluated in a rat model of Parkinson's disease induced through bilateral 6-hydroxydopamine lesions of the substantia nigra. In this model, AC-186 prevented motor, cognitive, and sensorimotor gating deficits and mitigated the loss of dopamine neurons in the substantia nigra, in males, but not in females. Furthermore, in male rats, 17β-estradiol, which activates ERβ and ERα with equal potency, did not show the same neuroprotective benefits as AC-186[2].In male rats,AC-186 provided essentially complete reversal of Taxol-induced allodynia at doses of 10 and 30 mg/kg. Repeat dosing experiments showed that no tolerance or desensitization to the effects of AC-186 occurred over 5 days. The analgesic effects of AC-186 were blocked by the ERβ-selective antagonist PHTPP, and coadministration of an ERα-selective agonist (PPT)[3].When ACP-105 is administered in combination with AC-186, they increase the amyloid-β degrading enzymes neprilysin and insulin-degrading enzyme and decrease amyloid-β levels in the brain as well as improve cognition. Interestingly, the androgen receptor level in the brain was increased by chronic treatment with the same combination treatment, ACP-105 and AC-186, not seen with DHT or ACP-105 alone[4]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00289380 | - | Recruiting | January 2020 | China, Beijing ... 展开 >> Beijing Friendship Hospital, Capital Medical University Active, not recruiting Beijing, Beijing, China, 100730 Peking Union Medical College Hospital Active, not recruiting Beijing, Beijing, China, 100730 China, Chongqing Chongqing Medical Univ. Hospital Completed Chongqing, Chongqing, China Xin Qiao Hospital Recruiting Chongqing, Chongqing, China Contact: Hua Yang, M.D. +86 13668057773 hyang@med.umich.edu Principal Investigator: Hua Yang, M.D. China, Guangdong The First Affiliated Hospital, Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510080 Contact: Wen-hua Zhan, M.D. +86 20 87755766 wenhuazhan@medmail.com.cn Principal Investigator: Wen-hua Zhan, M.D. Sub-Investigator: Xiao-qing Liu, M.D. China, Guangxi The First Affiliated Hospial, Guangxi Medical University Recruiting Nanning, Guangxi, China, 530021 Contact: Ning Xia, M.D. +86 771 5303201 Principal Investigator: Ning Xia, M.D. China, Hebei The First University Hospital, Hebei Medical University Recruiting Shijiazhuang, Hebei, China, 050031 Contact: Ru-mei Jia, M.D. +86 311 85917000 jiarm@jyyy.com.cn Principal Investigator: Ru-mei Jia, M.D. Nankai Hospital Active, not recruiting Tianjin, Hebei, China, 300100 China, Hubei Tongji Hospital, Huazhong University of Science and Technology Recruiting Wuhan, Hubei, China, 430030 Contact: Yi-ping Wu, M.D. +86 27 62363420 mail@tjh.tjmu.edu.cn Principal Investigator: Yi-ping Wu, M.D. China, Jiangsu Nanjing General Hospital of Nanjing Military Command Recruiting Nanjing, Jiangsu, China, 210002 Contact: Zhi-wei Jiang, M.D. +86 25 84619727 surgery34@163.com Principal Investigator: Zhi-wei Jiang, M.D. China, Shanghai Xin Hua Hospital, Shanghai Jiaotong University Recruiting Shanghai, Shanghai, China, 200029 Contact: Wei Cai, M.D. +86 21 65790000 caiwei204@yahoo.com.cn Principal Investigator: Wei Cai, M.D. Sixth Hospital Recruiting Shanghai, Shanghai, China Contact: Huai-Long Qin, M.D. hlqin@sjtu.edu.cn Sub-Investigator: Huai-Long Qin, M.D. China, Xinjiang The First Affiliated Hospital, Xinjiang Medical University Active, not recruiting Urumqi, Xinjiang, China, 830054 China, Zhejiang Second Affiliated Hospital, Zhejiang University Active, not recruiting Hangzhou, Zhejiang, China, 310006 收起 << | |
| NCT02798120 | Acne Vulgaris | Phase 3 | Completed | - | - |
| NCT03705507 | Acute Lymphoblastic Leukemia ... 展开 >> Acute Lymphoblastic Leukemia, Adult Acute Lymphoblastic Leukemia, Pediatric Acute Lymphoblastic Leukemia, in Relapse Acute Lymphoblastic Leukemia Recurrent 收起 << | Phase 1 Phase 2 | Recruiting | March 17, 2021 | United Kingdom ... 展开 >> Birmingham Children's Hospital Recruiting Birmingham, United Kingdom Principal Investigator: Alice Norton Alder Hey Children's Hospital Recruiting Liverpool, United Kingdom Principal Investigator: Mark Caswell Department of Paediatric Oncology, Royal Marsden Hospital, Sutton Recruiting London Borough of Sutton, United Kingdom Principal Investigator: Donna Lancaster Haemato-Oncology Adult Unit, Royal Marsden Hospital, Sutton Recruiting London Borough of Sutton, United Kingdom Sub-Investigator: David Taussig University College Hospital Recruiting London, United Kingdom Principal Investigator: Adele Fielding The Christie Hospital Recruiting Manchester, United Kingdom Principal Investigator: Anna Castleton Freeman Hospital Recruiting Newcastle, United Kingdom Sub-Investigator: Tobias Menne Great North Children's Hospital, Royal Victoria Infirmary Recruiting Newcastle, United Kingdom Principal Investigator: Geoff Shenton 收起 << |
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.26mL 0.65mL 0.33mL |
16.32mL 3.26mL 1.63mL |
32.65mL 6.53mL 3.26mL |
| 参考文献 |
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