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Dienogest

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Chemical Structure| 65928-58-7 同义名 : 地诺孕素 ;STS 557
CAS号 : 65928-58-7
货号 : A198037
分子式 : C20H25NO2
纯度 : 98%
分子量 : 311.418
MDL号 : MFCD00868356
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(80.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Progesterone receptor
描述 Dienogest is a specific progesterone receptor agonist with potent oral endometrial activity and is used in the treatment of endometriosis. It is available for use as an oral contraceptive in combination with ethinylestradiol. It has antiandrogenic activity and as a result can improve androgenic symptoms. It is a non-ethinylated progestin which is structurally related to testosterone[3]. Dienogest inhibits ovulation, produces secretory transformation of the endometrium and has antiproliferative effects. Oral dienogest 2 mg/day plus ethinylestradiol 30 micrograms/day provides effective contraception (Pearl Index approximately 0.2). Cycle stability is good during long term use of this combination; irregular vaginal bleeding was evident in 6% of women after 12 months' use. Androgenic symptoms (including hirsutism, seborrhoea, alopecia, acne vulgaris and hair and skin greasiness) improved in women treated with dienogest plus ethinylestradiol[4]. Dienogest 2 mg/day was superior to placebo in reducing pelvic pain, with similar results to buserelin, leuprorelin, leuprolide acetate and triptorelin, in controlling symptoms associated with endometriosis. Dienogest 2 mg/day was effective in reducing endometriotic lesions. The extended therapy with dienogest 2 mg/day also showed an improvement in pelvic pain after 24-52 weeks with tolerable side effects[5]. Dienogest 2 mg once daily is effective and safe in the long-term management of EAPP in Chinese women with endometriosis, with progressive decreases in EAPP (endometriosis-associated pelvic pain) and bleeding irregularities during continued treatment[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00280657 Acne Vulgaris Phase 3 Completed - -
NCT00764881 - Completed - -
NCT02636972 - Unknown January 2016 Australia, South Australia ... 展开 >> PARC, Royal Adelaide Hospital Adelaide, South Australia, Australia, 5000 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.11mL

6.42mL

3.21mL
参考文献

[1]Sasagawa S, Shimizu Y, et al. Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids. 2008 Feb;73(2):222-31.

[2]Okada H, Nakajima T, et al. The inhibitory effect of dienogest, a synthetic steroid, on the growth of human endometrial stromal cells in vitro. Mol Hum Reprod. 2001 Apr;7(4):341-7.

[3]Oettel M, Carol W, Gräser T, Klinger G, Mellinger U, Moore C, Schindler AE, Winkler UH. Der Einfluss einer Ethinylestradiol-Dienogest-Kombination auf die Serum-Androgen-Konzentrationen [Effect of ethinyl estradiol-dienogest combination on serum androgen concentrations]. Zentralbl Gynakol. 1997;119(12):597-606. German

[4]Foster RH, Wilde MI. Dienogest. Drugs. 1998 Nov;56(5):825-33; discussion 834-5

[5]Andres Mde P, Lopes LA, Baracat EC, Podgaec S. Dienogest in the treatment of endometriosis: systematic review. Arch Gynecol Obstet. 2015 Sep;292(3):523-9

[6]Yu Q, Zhang S, Li H, Wang P, Zvolanek M, Ren X, Dong L, Lang J. Dienogest for Treatment of Endometriosis in Women: A 28-Week, Open-Label, Extension Study. J Womens Health (Larchmt). 2019 Feb;28(2):170-177