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Norethindrone (Norethisterone; sold under many trade names) is a synthetic progestin that is taken orally to prevent pregnancy as an oral active contraceptive. It is also used to treat gynecological disorders and as part of menopausal hormone therapy.
| Targets |
Progesterone Receptor
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|---|---|
| ln Vitro |
Norethisterone, also known as 19-nortestosterone derivative, is primarily progestational rather than androgenic, with some oestrogenic and anti-oestrogenic activity. It lacks a C19 methyl group and has C17 ethinyl substitution. (Source: ) Progesterone receptor binding and transactivation activities are two times stronger in NET compared to Org 2058 (100%) and five to eight times weaker in NET. 3.2 and 1.1%, respectively, are the binding and transactivation activities of NET for the androgen receptor (5α-dihydrotestosterone 100%), none for the estrogen receptor (estradiol 100%), and below 1% for the glucocorticoid receptor (dexamethasone 100%).[2] Serum-stimulated or oestradiol (0.1 nM)-induced MCF-7 proliferation is inhibited by norethisterone (1 nM) by 41% and 34%, respectively.[/3] Significant effects on rat osteoblast proliferation, differentiation, and mineralization processes are induced by norethisterone (50 nM), which is mediated by the estrogen receptor and mimics the effects of estradiol.[4]
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| ln Vivo |
Norethisterone displays hormonal properties in vivo. MNorethisterone s.c.'smeanactive dose (MAD) in the progestagenic test (McPhail), androgenic test (Hershberger), estrogenic test (Allen–Doisy), and in a progestagenic and estrogenic test (ovulation inhibition test) is, respectively, 0.63 mg/kg, 2.5 mg/kg, 4 mg/kg, and 0.235 mg/kg.When taken orally, the MAD is 0.25 mg/kg, 20 mg/kg, 8 mg/kg, and 12 mg/kg. **[2]** Both bone resorption and formation are influenced by norethisterone. In SO and OVX mice, norethisterone (80 μg/day) reduced bone resorption while promoting estradiol-stimulated endosteal bone formation. (5) In castrated mice, norethisterone at the dose used in hormonal therapy for osteoporosis prevention has a minor protective effect against bone mineral loss. (6)
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| Cell Assay |
In assay kit medium, 96-well plates are seeded with roughly 1000 MCF-7 cells per well. The cells are then incubated for three days in a medium containing serum that has been treated with dextran and charcoal. After that, the wells are filled solely with norethisterone, and they are incubated for seven days. The cells are treated with a combination of 0.1 nM oestradiol and 0.1 nM norethisterone for seven days in order to simulate continuous combined HRT. An ATP-chemosensitivity test is used to quantify cell proliferation following a seven-day incubation period. To put it briefly, the bioluminescence reaction of luciferine in the presence of ATP and luciferase is measured to determine the amount of light emitted during proliferation.
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| Animal Protocol |
Rats: Individual caged Sprague-Dawley female rats (200-210 g), with six of them acting as controls, are housed in a brightly lit animal room from 9:00 a.m. to 9:00 p.m. For two weeks, each of the seven rats given norethindrone acetate is fed 35 μg per day. There is an abundance of water and the high-carb rat chow available.
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| References |
| Molecular Formula |
C20H26O2
|
|---|---|
| Molecular Weight |
298.4192
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| Exact Mass |
298.19
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| Elemental Analysis |
C, 80.50; H, 8.78; O, 10.72
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| CAS # |
68-22-4
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| Related CAS # |
Norethindrone (Standard);68-22-4;Norethindrone-d6;2376036-05-2
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| Appearance |
Solid powder
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| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@]2(C#C)O)CCC4=CC(=O)CC[C@H]34
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| InChi Key |
VIKNJXKGJWUCNN-XGXHKTLJSA-N
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| InChi Code |
InChI=1S/C20H26O2/c1-3-20(22)11-9-18-17-6-4-13-12-14(21)5-7-15(13)16(17)8-10-19(18,20)2/h1,12,15-18,22H,4-11H2,2H3/t15-,16+,17+,18-,19-,20-/m0/s1
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| Chemical Name |
(8R,9S,10R,13S,14S,17R)-17-ethynyl-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
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| Synonyms |
Utovlan; Norethindrone; 19-nor-17α-ethynyltestosterone; Norethisterone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25~60 mg/mL (83.8~201.1 mM)
Ethanol: ~5 mg/mL (~16.8 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.38 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3510 mL | 16.7549 mL | 33.5098 mL | |
| 5 mM | 0.6702 mL | 3.3510 mL | 6.7020 mL | |
| 10 mM | 0.3351 mL | 1.6755 mL | 3.3510 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05293574 | Not yet recruiting | Drug: norethisterone acetate | Ovarian Cyst Simple | Assiut University | October 1, 2022 | Phase 4 |
| NCT05916469 | Not yet recruiting | Drug: Norethindrone Acetate Drug: Levonorgestrel Intrauterine System |
Bleeding Disorder Von Willebrand Diseases |
Oregon Health and Science University |
July 2024 | |
| NCT04676061 | Recruiting | Drug: Norethindrone acetate (NTA) Drug: Placebo |
Implant Contraception |
Baylor Research Institute | February 11, 2021 | Phase 4 |
| NCT03271489 | Active Recruiting |
Drug: Elagolix Drug: E2/NETA |
Uterine Fibroids Heavy Menstrual Bleeding |
AbbVie | September 13, 2017 | Phase 3 |
| NCT04948489 | Not yet recruiting | Drug: norethindrone acetate (NETA) Drug: Placebo |
Endometriosis | Boston Children's Hospital | January 1, 2024 | Phase 2 |
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