| 公司名称： |
Wuhan NCE Biomedical Co.,Ltd. |
| 联系电话： |
4000-027-021 |24 hour enquiry :+86-13986109188 |English:+86-15623472865 |Japanese:+81-08033611988 |
| 产品介绍： |
英文名称:TAK-700
CAS:426219-18-3
纯度：99% HPLC 包装信息：50Mg,100Mg,500Mg,1g,5g,10g,50g,100g,500g,1kg 备注：XYA1181 |
| 公司名称： |
上海皓元化学科技有限公司 |
| 联系电话： |
86-21-58998590 |
| 产品介绍： |
英文名称:TAK-700
CAS:426219-18-3
纯度：>98% 包装信息：5Mg;10Mg;100Mg |
| 公司名称： |
上海阿拉丁生化科技股份有限公司 |
| 联系电话： |
021-20337333/400-620-6333 |
| 产品介绍： |
英文名称:TAK-700 (Orteronel)
CAS:426219-18-3
纯度：99% 包装信息：5MG,25MG |
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| 中文名称: | TAK-700 (ORTERONEL) | | 中文同义词: | 6-(6,7-二氢-7-羟基-5H-吡咯并[1,2-C]咪唑-7-基)-N-甲基-2-萘羧酰胺;6-[7-羟基-6,7-二氢-5H-吡咯并[1,2-C]咪唑-7-基]-N-甲基-2-萘甲酰胺 | | 英文名称: | TAK-700 | | 英文同义词: | 6-[7-Hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl]-N-methyl-2-naphthalenecarboxamide;(S)-6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-e]imidazol-7-yl)-N-methyl-2-naphthamide;6-[7-Hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl]-N-methyl-2-naphthalenecarboxamide TAK-700 (Orteronel) | | CAS号: | 426219-18-3 | | 分子式: | C18H17N3O2 | | 分子量: | 307.34648 | | EINECS号: | | | 相关类别: | Inhibitor |
| 生物活性 | TAK-700 (Orteronel)是一种有效的，高度选择性的，人17，20-lyase抑制剂，IC50为38 nM，比作用于其他CYPs(例如11-羟化酶和CYP3A4)选择性高1000倍以上。Phase 3。 | | 体外研究 | In vitro, TAK-700 shows the potent inhibitory activity against rat and human steroid 17,20-lyase inhibitor with IC50 of 54 nM and 38 nM, respectively. While other CYP isoforms including 11-hydroxylase and CYP3A4 are not significantly affected by TAK-700. In microsomes expressing human CYP isoforms, TAK-700 exhibit greater inhibitory effects on 17,20-lyase with IC50 of 19 nM compared to the other CYP isoforms. TAK-700 shows the inhibitory activity against monkey 17,20-lyase and 17-hydroxylase with IC50 of 27 nM and 38 nM, respectively. In monkey adrenal cells, TAK-700 inhibits the ACTH stimulated production of DHEA and androstenedione with IC50 of 110 nM and 130 nM, respectively. Moreover, TAK-700 also potently inhibits DHEA production in human adrenocortical tumor line H295R cells with IC50 of 37 nM. | | 体内研究 | In cynomolgus monkeys, oral treatment of TAK-700 at a dose of 1 mg/kg markedly reduces serum testosterone and dehydroepiandrosterone (DHEA) levels. Oral treatment of TAK-700 at a dose of 1 mg/kg results in favorable pharmacokinetic parameters with Tmax, Cmax, t1/2 and AUC0-24 hours of 1.7 hours, 0.147 μg/mL, 3.8 hours and 0.727 μg h/mL, respectively. |
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