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Norethindrone acetate (NSC-22844; NSC22844; NSC 22844; ENTA) is the 17-O-acetylated ester of Norethindrone (Norethisterone; sold under many trade names), which is a synthetic progestin and an orally active contraceptive for preventing pregnancy.
| ln Vivo |
For the treatment of symptomatic endometriosis, norethindrone acetate may be a reasonably priced substitute with manageable side effects. Dysmenorrhea and non-cyclic pelvic discomfort were relieved in norethindrone acetate-treated subjects [1]. For managing pain and bleeding in all phases of endometriosis, norethindrone acetate alone is a well-tolerated and efficient treatment. Norethindrone acetate medication improved bleeding scores regardless of prior hormonal regimen, and it also improved pain scores in all patients except those who had previously been treated a GnRH agonist + add-back [2]. In laboratory animals, norethindrone acetate shows little acute toxicity, which is in line with the absence of toxicity seen in people. When norethindrone acetate was given to rodents at multiple human doses, there was no observed treatment-related mortality, hematological alteration, behavioral alteration, or organ disease [3]. When rats fed a high-carb diet were given norethindrone acetate, their plasma lipoprotein densities (<1.006) and phospholipid concentrations of cholesterol, triglycerides, and plasma lipoproteins decreased significantly and proportionately. Significantly less palmitate and glycerol uptake was observed in triglycerides given to isolated rat hepatocytes when norethindrone acetate (0.1 mM) was administered [4].
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| References |
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| Additional Infomation |
According to state or federal labeling requirements, norethindrone acetate may cause developmental toxicity. Norethindrone acetate is a 3-oxoΔ(4)-steroid, a compound formed by the conversion of the hydroxyl group of norethindrone to acetate. It is a synthetic oral contraceptive and progestin. It is a 3-oxoΔ(4)-steroid, a terminal alkyne compound, and an acetate. Its function is related to norethindrone. Norethindrone acetate is the more bioavailable acetate of norethindrone, a synthetic progestin with certain anabolic, estrogenic, and androgenic activities. Like all progestins, norethindrone binds to and activates nuclear progesterone receptors (PR) in target tissues such as the pituitary gland and reproductive system; the ligand-receptor complex translocates to the nucleus, binds to the progesterone response element (PRE) on target genes, and subsequently triggers a series of transcriptional events and histone acetylation. Its physiological effects include inhibition of luteinizing hormone (LH) release, prolongation of the luteal phase of the endometrium, and alteration of cervical mucus secretion. Norethindrone acetate is a long-term contraceptive. See also: Norethindrone (active ingredient); Estradiol; Norethindrone acetate (ingredient); Leuprorelin acetate; Norethindrone acetate (ingredient)... See more...
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| Molecular Formula |
C22H28O3
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|---|---|
| Molecular Weight |
340.46
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| Exact Mass |
340.203
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| CAS # |
51-98-9
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| Related CAS # |
Norethindrone acetate-d8
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| PubChem CID |
5832
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
454.7±45.0 °C at 760 mmHg
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| Flash Point |
197.1±28.8 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.556
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| LogP |
3.99
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
695
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(=O)O[C@]1(CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=CC(=O)CC[C@H]34)C)C#C
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| InChi Key |
IMONTRJLAWHYGT-ZCPXKWAGSA-N
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| InChi Code |
InChI=1S/C22H28O3/c1-4-22(25-14(2)23)12-10-20-19-7-5-15-13-16(24)6-8-17(15)18(19)9-11-21(20,22)3/h1,13,17-20H,5-12H2,2-3H3/t17-,18+,19+,20-,21-,22-/m0/s1
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| Chemical Name |
[(8R,9S,10R,13S,14S,17R)-17-ethynyl-13-methyl-3-oxo-1,2,6,7,8,9,10,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-17-yl] acetate
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| Synonyms |
NSC-22844 NSC22844NSC 22844ENTA Norethindrone acetate
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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 : ≥ 100 mg/mL (~293.72 mM)
H2O : ~0.67 mg/mL (~1.97 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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 (7.34 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 (7.34 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 | 2.9372 mL | 14.6860 mL | 29.3720 mL | |
| 5 mM | 0.5874 mL | 2.9372 mL | 5.8744 mL | |
| 10 mM | 0.2937 mL | 1.4686 mL | 2.9372 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.
The Effect of Dienogest vs. Norethindrone Acetate Treatment in Endometriosis
CTID: NCT05476172
Phase: N/A Status: Completed
Date: 2023-07-21
Products are for research use only; We do not sell to patients
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