Etonogestrel

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Chemical Structure| 54048-10-1 同义名 : 3-keto-Desogestrel; 3-Oxodesogestrel; Etonogestrel, Implanon, nexplanon, 3-keto-desogestrel, 3-ketodesogestrel, 3-oxo desogestrel, 3-oxodesogestrel; ORG 3236; Nexplanon; Implanon
CAS号 : 54048-10-1
货号 : A190908
分子式 : C22H28O2
纯度 : 98%
分子量 : 324.46
MDL号 : MFCD00867863
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(154.1 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
描述 Etonogestrel is a synthetic form of the naturally occurring female sex hormone progesterone. It binds to the cytoplasmic progesterone receptors in the reproductive system and subsequently activates progesterone receptor mediated gene expression. FKBP51 is a repressor of PR/GR transcriptional activity, whose protein level are increased significantly in human endometrial stromal cells (HESCs) in response to estradiol (10−8 M) + etonogestrel (10−7 M) or estradiol + medroxyprogesterone acetate (10−7 M), but not to estradiol + progesterone (10−7 M)[3]. Etonogestrel subcutaneous implants in rats increased apoptotic index and Hscore values in stroma and glandular epithelium of uterus, granulosa and teca-lutein cells of the ovary with the longer progesterone exposure[4].
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
NCT03264781 Uterine Bleeding Phase 1 Phase 2 Recruiting December 2017 Thailand ... 展开 >> Chulalongkorn Hospital Recruiting Bangkok, Thailand Contact: Nitisa Tapanwong, MD       nitisa.tapanwong@gmail.com 收起 <<
NCT02367833 Bone; Disorder, Development an... 展开 >>d Growth 收起 << Phase 4 Active, not recruiting December 2018 United States, Pennsylvania ... 展开 >> Women's Health and Exercise Laboratories, The Pennsylvania State University University Park, Pennsylvania, United States, 16802 收起 <<
NCT01174225 Contraception Phase 4 Active, not recruiting December 2020 Canada, British Columbia ... 展开 >> Kelowna Womens' Clinic Kelowna, British Columbia, Canada 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.41mL

3.08mL

1.54mL

30.82mL

6.16mL

3.08mL

参考文献

[1]Tasdemir N, Kilic S, et al. Time dependent influence of etonogestrel on the caspase-3 immunoreactivity and apoptotic indexes of rat uterus and ovaries. Gynecol Endocrinol. 2012 Jun;28(6):463-7.

[2]Guzeloglu Kayisli O, Kayisli UA, et al. Progestins Upregulate FKBP51 Expression in Human Endometrial Stromal Cells to Induce Functional Progesterone and Glucocorticoid Withdrawal: Implications for Contraceptive- Associated Abnormal Uterine Bleeding. PLoS One. 2015 Oct 5;10(10):e0137855.

[3]Guzeloglu Kayisli O, Kayisli UA, Basar M, Semerci N, Schatz F, Lockwood CJ. Progestins Upregulate FKBP51 Expression in Human Endometrial Stromal Cells to Induce Functional Progesterone and Glucocorticoid Withdrawal: Implications for Contraceptive- Associated Abnormal Uterine Bleeding. PLoS One. 2015 Oct 5;10(10):e0137855. doi: 10.1371/journal.pone.0137855. PMID: 26436918; PMCID: PMC4593551.

[4]Tasdemir N, Kilic S, Lortlar N, Yuksel B, Goker U, Ozaksit G. Time dependent influence of etonogestrel on the caspase-3 immunoreactivity and apoptotic indexes of rat uterus and ovaries. Gynecol Endocrinol. 2012 Jun;28(6):463-7. doi: 10.3109/09513590.2011.633652. Epub 2012 Feb 17. PMID: 22578029.