| 常用名 | Tanaproget | CAS号 | 304853-42-7 |
|---|---|---|---|
| 价格 | ¥1660.0/5mg ¥7265.0/25mg ¥需询单/1g ¥3070.0/10mg | 纯度 | 99.0% |
| 备货期 | 1天 | 库存 | 现货 |
| 产品网页 | http://www.aladdin-e.com/zh_cn/T125113.html | ||
| 产品详情(用途,包装等)
用途: Tanaproget(NSP989) is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins.IC50 value: 0.1 nM (EC50, induce alkaline phosphatase activity) [1]Target: progesterone receptorTanaproget represents a potential first-in-class nonsteroidal PR agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.in vitro: In T47D cells, TNPR induces alkaline phosphatase activity with an EC(50) value of 0.1 nm, comparable with potent steroidal progestins such as medroxyprogesterone acetate (MPA) and trimegestone (TMG), albeit with a reduced efficacy ( approximately 60%). In a mammalian two-hybrid assay to measure PR agonist-induced interaction between steroid receptor co-activator-1 and PR, TNPR showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].in vivo: TNPR effectively down-regulated MMP expression in vitro and induced significant reduction of lesions in mice with disease established by tissues from endometriosis patients [2]. The maximum concentration (C(max)) of tanaproget occurred approximately 2 to 3 h after administration. The elimination half-life (t(1/2)) ranged from 12 to 30 h, and the oral clearance was approximately 70 L/h. The pharmacokinetics of tanaproget was not noticeably altered with a high-fat meal [3].Toxicity: All doses of tanaproget decreased cervical mucus scores (using a modified Insler method), indicating poor production and poor quality of cervical mucus. The most frequent treatment-emergent adverse events were vaginal bleeding/spotting, abdominal cramping and vomiting; their incidence was not dose related and most events were mild [3]. 物理化学性质: CAS号:304853-42-7 常用中文名:Tanaproget 常用英文名:Tanaproget 分子式:C16H15N3OS 分子量:297.37500 密度:N/A 沸点:N/A 熔点:N/A 闪点:N/A 储存条件:2-8℃ |