| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T409119-1ml |
1ml |
现货  |
|
| 英文别名 | (S)-6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-e]imidazol-7-yl)-N-methyl-2-naphthamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | TAK-700 (Orteronel) |
| 生化机理 | TAK-700（Orteronel）是一种强效、高选择性的人类 17,20-lyase 抑制剂，IC50 为 38 nM，与其他 CYPs（如 11-hydroxylase 和 CYP3A4）相比，具有大于 1000 倍的选择性。TAK-700（Orteronel）是一种雄激素生物合成抑制剂。第 3 阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
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。TAK-700 (Orteronel) 是一种雄性激素 androgen 生物合成抑制剂。 Information TAK-700 (Orteronel) is a potent and highly selective human17,20-lyaseinhibitor withIC50of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). TAK-700 (Orteronel) is anandrogenbiosynthesis inhibitor. Phase 3. In vitro, TAK-700 shows the potent inhibitory activity against rat and human steroid 17,20-lyase 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. In vivo 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. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CNC(=O)C1=CC2=C(C=C1)C=C(C=C2)C3(CCN4C3=CN=C4)O |
| 分子量 | 307.35 |
| Reaxy-Rn | 11851093 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11851093&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 57 mg/mL (200.53 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| 象形图 | GHS08 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H372: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子 |
| 预防措施声明 |
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。 |
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