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(-)-Norgestrel/左炔诺孕酮 {[allProObj[0].p_purity_real_show]}

货号:A422801 同义名: D-(-)-炔诺孕酮 / D-Norgestrel; Levonorgestrel

(-)-Norgestrel是一种合成孕激素,作为一些激素避孕药的活性成分,作用于孕酮受体。

(-)-Norgestrel/左炔诺孕酮 化学结构 CAS号:797-63-7
(-)-Norgestrel/左炔诺孕酮 化学结构
CAS号:797-63-7
(-)-Norgestrel/左炔诺孕酮 3D分子结构
CAS号:797-63-7
(-)-Norgestrel/左炔诺孕酮 化学结构 CAS号:797-63-7
(-)-Norgestrel/左炔诺孕酮 3D分子结构 CAS号:797-63-7
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(-)-Norgestrel/左炔诺孕酮 纯度/质量文件 产品仅供科研

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(-)-Norgestrel/左炔诺孕酮 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].

(-)-Norgestrel/左炔诺孕酮 细胞实验

Cell Line
Concentration Treated Time Description References
Human fallopian tube epithelial cells 25 nM 4 hours To assess the effect of levonorgestrel on sperm function, results showed no significant effect on sperm count, adhesion, or acrosome reaction rate Reprod Biol Endocrinol. 2012 Jan 30;10:8.

(-)-Norgestrel/左炔诺孕酮 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Pigtailed macaques Pigtailed macaque model Vaginal administration 0.536 mg/IVR Single administration, lasting 28 days To evaluate the safety and pharmacokinetics of the MPT IVR in pigtailed macaques, results showed the IVR was safe and well tolerated with sustained release of all APIs over 28 days. J Control Release. 2024 Dec;376:1209-1224
Sprague-Dawley rats Implantable PLGA microneedles Subcutaneous implantation 500 μg/rat Single administration, observed for 13-16 days Evaluate the pharmacokinetics and release behavior of (-)-Norgestrel in vivo. Results showed that PLGA microneedles with 33.3% trehalose released faster, maintaining contraceptive effect for 13 days, while those without trehalose maintained for 16 days. Polymers (Basel). 2020 Jan 1;12(1):59

(-)-Norgestrel/左炔诺孕酮 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 - -

(-)-Norgestrel/左炔诺孕酮 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

(-)-Norgestrel/左炔诺孕酮 实验方案

计算器
存储液制备 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

(-)-Norgestrel/左炔诺孕酮 技术信息

CAS号797-63-7
分子式C21H28O2
分子量 312.45
SMILES Code O=C1CC[C@]2([H])[C@@]3([H])CC[C@]4(CC)[C@@](C#C)(O)CC[C@@]4([H])[C@]3([H])CCC2=C1
MDL No. MFCD00199013
别名 D-(-)-炔诺孕酮 ;D-Norgestrel; Levonorgestrel; Levonorgestrel, Norgestrel, Microval, Postinor, Mirena, Plan B
运输蓝冰
InChI Key WWYNJERNGUHSAO-XUDSTZEESA-N
Pubchem ID 13109
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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