Levonorgestrel |
Catalog No.GC14704
One-Click Copy Product Info
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Levonorgestrel is an effective oral progesterone inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 797-63-7
Sample solution is provided at 25 µL, 10mM.
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Levonorgestrel is an effective oral progesterone inhibitor [1]. Levonorgestrel can be used for contraception and can be combined with other drugs. Levonorgestrel has anti-cancer activity and can induce cell apoptosis, and is used in the research of osteoporosis and uterine leiomyoma [2].
In vitro, Levonorgestrel (5-25μg/mL; 72h) can inhibit cell proliferation and promote cell apoptosis in uterine smooth muscle tumor cells in a concentration-dependent manner. It can significantly reduce the expression of Bcl-2 and Survivin, increase the phosphorylation level of p38, and activate caspase 3 [2]. Levonorgestrel (50μM) has a time-dependent inhibitory effect on the proliferation of HESCs and HEGCs, and significantly increases cell apoptosis. Levonorgestrel causes a time-dependent increase in the total Cx43 content, but does not cause changes in Ser368 phosphorylated Cx43, while Ser255 phosphorylated Cx43 shows a nuclear translocation phenomenon [3].
In vivo, after random mating in mice, Levonorgestrel (8mg/kg) isintraperitoneally injected immediately, and the frequency of ciliary beating of the fallopian tubes (CBF) in mice decreases significantly. The average percentage of embryo-tube retention in the Levonorgestrel group is 18.27% [4]. Oral administration of Levonorgestrel (0.67mg/kg/day) and quinestrol for 7 days significantly reduces sperm count in SD rats and decreases androgen receptor and Wilms tumor nuclear protein 1 (WT1) staining. Quinestrolalone or in combination with Levonorgestrel induces low fertility in male rats, primarily by interfering with reproductive cell differentiation [5].
References:
[1] Tellería CM, Carrizo DG, Deis RP. Levonorgestrel inhibits luteinizing hormone-stimulated progesterone production in rat luteal cells. J Steroid Biochem Mol Biol. 1994 Aug;50(3-4):161-6.
[2] Xu Qing, et al. Levonorgestrel inhibits proliferation and induces apoptosis in uterine leiomyoma cells. Contraception vol. 82,3 (2010): 301-8.
[3] Zhao X, Tang X, Ma T, et al. Levonorgestrel inhibits human endometrial cell proliferation through the upregulation of gap junctional intercellular communication via the nuclear translocation of Ser255 phosphorylated Cx43[J]. BioMed Research International, 2015, 2015(1): 758684.
[4] Li C, Zhang H Y, Liang Y, et al. Effects of Levonorgestrel and progesterone on Oviductal physiology in mammals[J]. Reproductive Biology and Endocrinology, 2018, 16(1): 59.
[5] Liu M, Wan X, Yin Y, et al. Subfertile effects of quinestrol and levonorgestrel in male rats[J]. Reproduction, Fertility and Development, 2012, 24(2): 297-308.
| Cell experiment [1]: | |
Cell lines | Human endometrial stromal cells (HESCs) and glandular cells (HEGCs) |
Preparation Method | HESCs and HEGCs were placed in 200 μl of culture media per well in a 96-well plate with a density of 2 × 104 cells/mL and incubated overnight to allow the cells to attach to the wells. The cells were then treated with 2 μL of Levonorgestrel in a concentration course manner (1×10−3, 10, 25, or 50μM) and in a time course (24h, 48h, and 72h), with Estradiol (E2) as the opposite control, and DMSO (0.5%) as the negative control. The concentration of Levonorgestrel displaying an inhibitory effect and that of E2 exhibiting a stimulatory effect on cell proliferation (both were 50μM) were adopted as the final treating concentrations during the followed experiments determined according to the preliminary experiments. The concentration of 50μM Levonorgestrel is similar to that in the vivo endometrium in the presence of a mirena with a releasing rate of 20 μg/24 hours of Levonorgestrel. Subsequently, the MTT method was used for detection. |
Reaction Conditions | 1×10−3, 10, 25, or 50μM ; 24h, 48h and 72h |
Applications | 50μM Levonorgestrel inhibited the cell proliferation of primary HESCs significantly over time (24h, 48h, and 72h). |
| Animal experiment [2]: | |
Animal models | C57BL/6 |
Preparation Method | Eight-week-old C57BL/6 J mice were used in this study (Shanghai Research Center for Model Organisms). All animal experiments were approved by the Medical Ethics Committee of Shanghai Research Center for Model Organisms. The mice were housed in a room at 25°C with a 12-h light:12-hdark cycle and 50–60% humidity and were given a standard diet (containing 10% fat) and water. Female mice (6–8 weeks of age) were mated randomly, and vaginal plug-positive mice were immediately injected intraperitoneally with saline, Levonorgestrel (8mg/kg), or Progesterone (8mg/kg). Twelve hours after observation of the vaginal plug, the mice were sacrificed via cervical dislocation to measure the CBF. Embryo-tube transportation assays were conducted as described by Ning et al. Seventy-four hours after observation of the vaginal plug, the oviducts and uterus were ligated. The embryos were flushed from the oviducts or uteri with PBS. We counted the embryos remaining in the oviducts, and the results are expressed as percentages of the total number of embryos. |
Dosage form | 8mg/kg once; i.p. |
Applications | All the mice in the Levonorgestrel group experienced embryo-tube retention, with an average percentage of embryo retention of 18.27%, whereas none of the mice in the saline-treated group experienced embryo-tube retention. Consistently, the same effect was also observed in the Progesterone group, which had an average percentage of embryo retention of 15.37%, compared with the control group, which had an average percentage of 0%. |
References: | |
| Cas No. | 797-63-7 | SDF | |
| Chemical Name | (8R,9S,10R,13S,14S,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one | ||
| Canonical SMILES | CCC12CCC3C(C1CCC2(C#C)O)CCC4=CC(=O)CCC34 | ||
| Formula | C21H28O2 | M.Wt | 312.45 |
| Solubility | ≥ 13.8mg/mL in DMSO | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2005 mL | 16.0026 mL | 32.0051 mL |
| 5 mM | 640.1 μL | 3.2005 mL | 6.401 mL |
| 10 mM | 320.1 μL | 1.6003 mL | 3.2005 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)