Home Endocrinology & Hormones Progesterone Receptor chemical - - Other chemical Norethindrone

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Norethindrone Progesterone Receptor chemical

Cat.No.S4040

Norethindrone (Norethisterone) is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
Norethindrone Progesterone Receptor chemical Chemical Structure

Chemical Structure

Molecular Weight: 298.42

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Batch: S404001 DMSO]60 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.79%
99.79

Chemical Information, Storage & Stability

Molecular Weight 298.42 Formula

C20H26O2

 Storage (From the date of receipt)
CAS No. 68-22-4 Download SDF Storage of Stock Solutions

Synonyms Norethisterone Smiles CC12CCC3C(C1CCC2(C#C)O)CCC4=CC(=O)CCC34

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (201.05 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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 ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

In vitro
Norethisterone, or, is a 19-nortestosterone derivative, that lacks a C19 methyl group and possesses C17 ethinyl substitution, and primarily displays progestational activity rather than androgenic activity and, to a lesser extent, has oestrogenic and anti-oestrogenic activity. [1] NET shows five- to eight-fold weaker progesterone receptor binding and transactivation activities than the Org 2058 (100%) and two-fold stronger than progesterone. Binding and transactivation activities of NET for androgen receptor (5α-dihydrotestosterone 100%) are 3.2 and 1.1%, respectively, for estrogen receptor none (estradiol 100%) and for glucocorticoid receptor below 1% (dexamethasone 100%). [2] Norethisterone (1 nM) inhibits serum-stimulated or oestradiol (0.1 nM)-induced proliferation of MCF-7 by 41% and 34%, respectively. [3] Norethisterone (50 nM) induces significant effects on rat osteoblast proliferation, differentiation, and mineralization processes, mimicking the effects of estradiol, which is mediated by estrogen receptor. [4]
In vivo
Norethisterone displays hormonal properties in vivo. Mean active dose (MAD) of Norethisterone s.c. in progestagenic test (McPhail), androgenic test (Hershberger), estrogenic test (Allen–Doisy), and in a progestagenic and estrogenic test (ovulation inhibition test) is 0.63 mg/kg, 2.5 mg/kg, 4 mg/kg, and 0.235 mg/kg, respectively, and the MAD for orally administration is 0.25 mg/kg, 20 mg/kg, 8 mg/kg, and 12 mg/kg, respectively. [2] Norethisterone influences bone formation and resorption. Norethisterone (80 μg/day) decreased bone resorption in SO and OVX mice, while enhances estradiol-stimulated endosteal bone formation. [5] Norethisterone at the dose which is used in hormonal therapy for prevention of osteoporosis has a slight protective effect against bone mineral loss in castrated mice. [6]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17535886/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8442440/
  • [6] https://pubmed.ncbi.nlm.nih.gov/17402553/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05293574 Unknown status
Ovarian Cyst Simple
Assiut University
 October 1 2022 Phase 4
NCT05294341 Completed
Contraception
Milton S. Hershey Medical Center
 July 22 2022 Phase 4
NCT04016753 Completed
Healthy Participants
Bristol-Myers Squibb
 August 5 2019 Phase 1
NCT02905890 Completed
Bacterial Vaginosis|HIV
London School of Hygiene and Tropical Medicine|Imperial College London|University of Liverpool|MRC/UVRI and LSHTM Uganda Research Unit
 October 2 2017 Phase 4

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