TAK-700 R-form

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

可选规格

包装

价格

促销价

数量
5mg

￥1087.00

869.00

- +
10mg

￥1675.00

1340.00

- +
50mg

￥6620.00

5296.00

- +
200mg

￥18960.00

15168.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

17, 20-lyase inhibitor

货号：ajci14064
CAS：752243-39-3
分子式：C18H17N3O2
分子量：307.35
纯度：98%
存储：Store at -20°C
库存：现货

Background:

TAK-700 R-form is a highly selective inhibitor of 17, 20-lyase with IC50 value of 38nM [1].

TAK-700 is a potent and selective inhibitor of the 17, 20-lyase activity of CYP17A1 which is responsible for androgen biosynthesis. Thus, TAK-700 is selected as a candidate for treatment of prostate cancer through reducing the adrenal androgen production. As an inhibitor of CYP17A1, the selectivity of TAK-700 is important to avoid causing the drug–drug interactions or side effects. TAK-700 shows potent inhibitory activity and high selectivity against 17, 20-lyase over other CYPs including 11-hydroxylase and CYP3A4. The IC50 values for 11-hydroxylase and CYP3A4 are above 1μM and above 10μM, respectively. Moreover, in a monkey model, the administration of TAK-700 is found to significantly reduce serum testosterone and DHEA levels [1].

参考文献:
[1] Kaku T, Hitaka T, Ojida A, et al. Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17, 20-lyase inhibitor with potential utility in the treatment of prostate cancer. Bioorganic & medicinal chemistry, 2011, 19(21): 6383-6399.