产品描述: | 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), |
体内研究: |
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 |
参考文献: |
1. Bapst JL, et al. Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women. Contraception. 2006 Nov;74(5):414-8. 2. Zhang Z, et al. Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget. J Biol Chem. 2005 Aug 5;280(31):28468-75. 3. Bruner-Tran KL, et al. Down-regulation of endometrial matrix metalloproteinase-3 and -7 expression in vitro and therapeutic regression of experimental endometriosis in vivo by a novel nonsteroidal progesterone receptor agonist, tanaproget. J Clin Endocrinol Metab. 2006 Apr;91(4):1554-60. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.363 ml |
16.814 ml |
33.628 ml |
5 mM |
0.673 ml |
3.363 ml |
6.726 ml |
10 mM |
0.336 ml |
1.681 ml |
3.363 ml |
50 mM |
0.067 ml |
0.336 ml |
0.673 ml |
|
注意: |
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