Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tanaproget 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: 0.1 nM),
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | 5 days | $ 112.00 | |
5 mg | 5 days | $ 197.00 | |
10 mg | 5 days | $ 297.00 | |
25 mg | 5 days | $ 615.00 | |
1 mL * 10 mM (in DMSO) | 5 days | $ 217.00 |
Description | Tanaproget 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: 0.1 nM), |
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 a significant reduction of lesions in mice with disease established by tissues from endometriosis patients. 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 [2][3]. |
Synonyms | NSP-989 |
Molecular Weight | 297.38 |
Formula | C16H15N3OS |
CAS No. | 304853-42-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (168.14 mM)
You can also refer to dose conversion for different animals. More
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Tanaproget 304853-42-7 Others NSP-989 NSP 989 NSP989 inhibitor inhibit