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Tanaproget

CAS No. : 304853-42-7

Biological Activity：Tanaproget (NSP-989) 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 receptor
Tanaproget 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].

Research Area：Endocrinology

Targets：Progesterone Receptor

Related Screening Libraries:Covalent Screening Library Plus;Bioactive Compound Library Plus;Covalent Screening Library;Endocrinology Compound Library;Nuclear Receptor Compound Library;

Related Small Molecules:Gestonorone Capronate;Chlormadinone acetate-d6-1;17α-Hydroxyprogesterone;Nestoron;Melengestrol acetate-d2;Asoprisnil-d3;Norgestrel-d6;Progesterone-13C2;Melengestrol acetate;Progesterone;Progesterone-13C5;PF-02413873;Chlormadinone acetate;Chlormadinone acetate-d6;ARD-61;Altrenogest

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