Licensed by Pfizer Catalog No.S1727
Molecular Weight(MW): 312.45
Levonorgestrel is a female hormone that prevents ovulation.
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Choose Selective Estrogen/progestogen Receptor Inhibitors
|Description||Levonorgestrel is a female hormone that prevents ovulation.|
Levonorgestrel suppresses the stimulation of progesterone secretion induced by oLH, dibutyryl-cAMP and Pregnenolone in rats luteal cells.  Levonorgestrel also inhibits constrictions evoked by either a high potassium (K(+)) solution or phorbol myristate acetate (PMA) in the absence and presence of extracellular calcium (Ca(2+)). Levonorgestrel depresses contractions evoked by Ca(2+) and reduces (45)Ca(2+) influx in depolarized veins. Levonorgestrel increases levels of cyclic AMP and inhibits PMA-induced activation of protein kinase C in veins. Levonorgestrel causes endothelium-independent relaxations of jugular veins via inhibition of Ca(2+) entry and of protein kinase Cactivation.  Levonorgestrel inhibition of both estrogen-induced pituitary weight increment and hyperprolactinemia is reduced by mifepristone, whereas Flutamide is unable to block Levonorgestrel effects 
|In vivo||Levonorgestrel down-regulates the mRNA expression of follicle-stimulating hormone receptor (FSHR), luteinizing hormone receptor (LHR), estrogen receptor (ER) β and progesterone receptor (PR) in the ovary, and ERα and PR in the uterus of Mongolian gerbils.  Levonorgestrel causes a significant upregulation of the mRNA expression of the gene encoding luteinising hormone β-subunit (lhβ) and the suppression of the mRNA expression of the gene encoding follicle-stimulating hormone β-subunit (fshβ) in the pituitary of both male and female roach. Levonorgestrel disrupts the reproductive system of pubertalroach by affecting the pituitary gonadotropin expression and the sex steroid levels in pubertal roach (Rutilus rutilus). |
-  Teller韆 CM, et al. J Steroid Biochem Mol Biol,?994, 50(3-4), 161-166.
-  Herkert O, et al. Br J Pharmacol,?000, 130(8), 1911-1918.
-  Rey-Rold醤 EB, et al. Horm Metab Res,?008, 40(4), 245-250.
|In vitro||DMSO||45 mg/mL (144.02 mM)|
|Ethanol||2 mg/mL (6.4 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03557619||Recruiting||Drug: Venetoclax|Drug: ethinyl estradiol/levonorgestrel||Hematologic Malignancies||AbbVie||July 30 2019||Phase 1|
|NCT03954366||Recruiting||Drug: Rucaparib|Drug: Rosuvastatin|Drug: Oral Contraceptives||Neoplasms||Clovis Oncology Inc.||May 8 2019||Phase 1|
|NCT03745144||Recruiting||Drug: Cladribine|Drug: Placebo|Drug: Microgynon®||Relapsing Multiple Sclerosis (RMS)||Merck KGaA Darmstadt Germany||January 17 2019||Phase 1|
|NCT03675581||Recruiting||Drug: Microgynon|Drug: Nintedanib||Scleroderma Systemic||Boehringer Ingelheim||November 8 2018||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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