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research use only
Cat.No.S1727
| Related Targets | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Other Estrogen/progestogen Receptor Inhibitors | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV471) MPP dihydrochloride Cholesterol Endoxifen HCl G15 Chrysin Licochalcone A AZD9496 PHTPP |
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In vitro |
DMSO
: 62 mg/mL
(198.43 mM)
Ethanol : 5 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 312.45 | Formula | C21H28O2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 797-63-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | D-Norgestrel | Smiles | CCC12CCC3C(C1CCC2(C#C)O)CCC4=CC(=O)CCC34 | ||
| Targets/IC50/Ki |
Progesterone receptor
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|---|---|
| In vitro |
Levonorgestrel suppresses the stimulation of progesterone secretion induced by oLH, dibutyryl-cAMP and Pregnenolone in rats luteal cells. This compound 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+)). It depresses contractions evoked by Ca(2+) and reduces (45)Ca(2+) influx in depolarized veins. The chemical increases levels of cyclic AMP and inhibits PMA-induced activation of protein kinase C in veins. It causes endothelium-independent relaxations of jugular veins via inhibition of Ca(2+) entry and of protein kinase Cactivation. Its inhibition of both estrogen-induced pituitary weight increment and hyperprolactinemia is reduced by mifepristone, whereas Flutamide is unable to block this compound's effects
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| 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. This compound 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. It disrupts the reproductive system of pubertalroach by affecting the pituitary gonadotropin expression and the sex steroid levels in pubertal roach (Rutilus rutilus).
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06380205 | Recruiting | Healthy Participants |
Incyte Corporation |
May 7 2024 | Phase 1 |
| NCT06188026 | Recruiting | Healthy Volunteers (Non-alcoholic Steatohepatitis) |
Novo Nordisk A/S |
December 18 2023 | Phase 1 |
| NCT05896384 | Recruiting | Healthy |
Boehringer Ingelheim |
December 7 2023 | Phase 1 |
| NCT05700812 | Recruiting | IUD|IUD Insertion Complication|IUD; Complications |
University of California Davis |
February 1 2023 | Not Applicable |
| NCT05671653 | Terminated | Obesity |
Pfizer |
January 19 2023 | Phase 1 |
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