Tanaproget, ≥99%
Product Name： Tanaproget
CAS號(hào):304853-42-7
分子式:C16H15N3OS
分子量:297.37
貯存： 儲(chǔ)存溫度-20°C
可溶性： 25°C： DMSO
生化和生理學(xué)機(jī)理：
Description：
IC50 Value： 0.1 nM (EC50, induce alkaline phosphatase activity) [1]
Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the VIP(pr) from various species with a higher relative affinity than reference steroidal progestins. Tanaproget represents a potential first-in-class nonsteroidal VIP(pr) agonist for contraception with improved safety and side effect profiles versus currently available steroidal oral contraceptives.
in vitro： In T47D cells, TNVIP(pr) 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 VIP(pr) agonist-induced interaction between steroid receptor co-activator-1 and VIP(pr), TNVIP(pr) showed similar potency (EC(50) value of 0.02 nm) and efficacy to MPA and TMG [1].
in vivo： TNVIP(pr) effectively down-regu
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