Tanaproget

Tanaproget is an orally effective, selective nonsteroidal progesterone receptor (PR) agonist targeting human PR with an IC₅₀ of 1.7 nM. Tanaproget promotes the interaction between PR receptors and coactivators (such as SRC-1), thereby inhibiting the secretion of matrix metalloproteinases (MMP-3/MMP-7) and reducing endometrial tissue invasion and angiogenesis. Tanaproget can be used for contraception and endometriosis inhibition research^[1][2][3]. In Vitro:Tanaproget (1 nM; 3-5 days) significantly down-regulated pro-MMP-3 expression in endometrial stromal cells isolated from normal women, even under IL-1α stimulation^[1].
Tanaproget (1-100 pM; 48-72 h) inhibited the secretion of pro-MMP-3 and pro-MMP-7 in endometrial organ cultures from exogenous endometriosis patients^[1].
Tanaproget (0.1 nM; 24 h) induced alkaline phosphatase activity in T47D cells with an EC₅₀ of 0.15 nM (human), which is comparable to steroidal progestins^[2].
Tanaproget against PR of different species with IC₅₀s of 1.7 nM (human), 0.3 nM (monkey), and 0.5 nM (rat, rabbit)^[2].
In Vivo:Tanaproget (300 μg/kg; gavage/sustained-release capsules; once daily; 14-16 days) significantly reduces the number and size of human endometriotic lesions in the ncr/nude mouse endometriosis model^[1].
Tanaproget (0.03 mg/kg; oral; once daily; 4 days) completely inhibits ovulation in the Sprague-Dawley rat ovulation inhibition model and is 30 times more potent than steroidal progestins^[2].