网站主页 > 化工产品目录 > 生物化工 > 抑制剂 > 代谢(Metabolism) > P450 (e.g. CYP17) 抑制剂 > TAK-700 (ORTERONEL)

TAK-700 (ORTERONEL)

TAK-700 (ORTERONEL) 更多供应商
公司名称:上海波以尔化工有限公司  
联系电话:86-15221043597
产品介绍:英文名称:Orteronel
CAS:426219-18-3
公司名称:BOC Sciences  
联系电话:
产品介绍:英文名称:TAK-700
CAS:426219-18-3
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:6155RMB/25MG 备注:试剂级
公司名称:广州爱纯医药科技有限公司  
联系电话:020-39119399 18927568969
产品介绍:英文名称:TAK700
CAS:426219-18-3
纯度:98% 包装信息:25mg; 100mg; 1g; 5g; 25g;100g 备注:现货
最新发布供应信息
TAK-700_上海贝昶生物科技有限公司
2013/4/23 15:17:10
TAK-700 (ORTERONEL)
生物活性 体外研究 体内研究
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:(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);6-(6,7-dihydro-7-hydroxy-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-Naphthalenecarboxamide;6-(6,7-dihydro-7-hydroxy-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methy;6-[7-Hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl]-N-methyl-2-naphthalenecarboxamide
CAS号:426219-18-3
分子式:C18H17N3O2
分子量:307.34648
EINECS号:
相关类别:Inhibitors;小分子抑制剂,天然产物;代谢;Inhibitor
Mol文件:426219-18-3.mol
TAK-700 (ORTERONEL)
TAK-700 (ORTERONEL) 性质
TAK-700 (ORTERONEL) 用途与合成方法
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.
安全信息
"TAK-700 (ORTERONEL)" 相关产品信息
PHA-665752 4-[4-(1,3-苯并二唑-5-基)-5-(2-吡啶基)-1H-咪唑-2-基]-苯酰胺水合物 N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺 Ferrostatin-1 (Fer-1) Obatoclax 甲磺酸盐 SU9516