(-)-Norgestrel

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Chemical Structure| 797-63-7 同义名 : D-(-)-炔诺孕酮 ;D-Norgestrel;Levonorgestrel;Levonorgestrel, Norgestrel, Microval, Postinor, Mirena, Plan B
CAS号 : 797-63-7
货号 : A422801
分子式 : C21H28O2
纯度 : 99+%
分子量 : 312.45
MDL号 : MFCD00199013
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(336.06 mM),配合低频超声,并水浴加热至45℃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 Levonorgestrel is a synthetic progestogen used as an active ingredient in some hormonal contraceptives. Approximately 20% of levonorgestrel intrauterine system users experience amenorrhea during at least 1 90-day interval by the first year after insertion[3]. Furthermore, when two doses of levonorgestrel 0.75 mg are administered, the second dose can confidently be taken 12-24 hours after the first without compromising efficacy[4]. In addition, the prevalence of adverse events after a levonorgestrel 0.75 mg two-dose regimen and a levonorgestrel 1.5 mg single-dose regimen were not statistically different[5]. Low-dose ethinylestradiol/levonorgestrel 20 microg/100 microg is a combined oral contraceptive that prevents pregnancy primarily by inhibiting ovulation. Ethinylestradiol/levonorgestrel 20 microg/100 microg is well tolerated; adverse events were those commonly associated with combined oral contraceptives[6]. The LNG-IUS (levonorgestrel-releasing intrauterine system) can be used successfully throughout the reproductive period for effective contraception and treatment of menorrhagia[7].
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
NCT01286948 Female Contraception Phase 1 Completed - Chile ... 展开 >> Instituto Chileno de Medicina Reproductiva José Victorino Lastarria 29, Santiago, Chile Dominican Republic Profamilia Socorro Sanchez No. 160, Santo Domingo, Dominican Republic, Apartado Postal 1053 收起 <<
NCT02545452 Endometriosis Phase 1 Completed - Germany ... 展开 >> Berlin, Germany, 13353 收起 <<
NCT02616146 Contraception Phase 3 Terminated - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.00mL

3.20mL

1.60mL

32.01mL

6.40mL

3.20mL

参考文献

[1]Herkert O, Kuhl H, et al. The progestin levonorgestrel induces endothelium-independent relaxation of rabbit jugular vein via inhibition of calcium entry and protein kinase C: role of cyclic AMP. Br J Pharmacol. 2000 Aug;130(8):1911-8.

[2]Telleria CM, Carrizo DG, et al. Levonorgestrel inhibits luteinizing hormone-stimulated progesterone production in rat luteal cells. J Steroid Biochem Mol Biol. 1994 Aug;50(3-4):161-6.

[3]Sergison JE, Maldonado LY, Gao X, Hubacher D. Levonorgestrel intrauterine system associated amenorrhea: a systematic review and metaanalysis. Am J Obstet Gynecol. 2019 May;220(5):440-448.e8

[4]Hansen LB, Saseen JJ, Teal SB. Levonorgestrel-only dosing strategies for emergency contraception. Pharmacotherapy. 2007 Feb;27(2):278-84

[5]Leelakanok N, Methaneethorn J. A Systematic Review and Meta-analysis of the Adverse Effects of Levonorgestrel Emergency Oral Contraceptive. Clin Drug Investig. 2020 May;40(5):395-420

[6]Dando TM, Curran MP. Low-dose ethinylestradiol/levonorgestrel. Drugs. 2005;65(16):2299-306; discusion 2307-8

[7]Andersson K. The levonorgestrel intrauterine system: more than a contraceptive. Eur J Contracept Reprod Health Care. 2001 Jan;6 Suppl 1:15-22