S84851 |
Tanaproget |
源叶(MedMol) | 99% |
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- 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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)