Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Segesterone acetate (formerly known as ST1435; ST-1435 or nestorone; trade name: Annovera) is a progesterone receptor agonist that is prescribed as a female contraceptive. In August 2018, the FDA approved a novel vaginal ring system that uses estradiol and semen to prevent pregnancy for a full year. Segesterone inhibits proinflammatory mediators and neuropathology in the wobbler mouse model of motoneuron degeneration as a female-contraceptive drug. Segesterone may have benefits for multiple sclerosis (MS) as it prevented hippocampal abnormalities and enhanced the functional outcomes of EAE mice.
Targets |
progesterone receptor (EC50 = 50.3 nM)
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ln Vivo |
Following Segesterone acetate (400 μCi 3H Nestoron/kg BW; subcutaneous injection; female Sprague-Dawley rats) treatment, the Cmax in plasma and blood is 95.5 and 58.1 ng equiv. 3H Nestoron/g, respectively, with a t1/2 of 15.6 hours. Feces and urine excrete about 81.4% and 7.62% of the dose that was administered, respectively[1].
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References |
Molecular Formula |
C23H30O4
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Molecular Weight |
370.49
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Exact Mass |
370.21
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Elemental Analysis |
C, 74.56; H, 8.16; O, 17.27
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CAS # |
7759-35-5
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Related CAS # |
7690-08-6;7759-35-5 (acetate);
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Appearance |
Solid powder
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SMILES |
CC(=O)[C@]1(C(=C)C[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=CC(=O)CC[C@H]34)C)OC(=O)C
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InChi Key |
CKFBRGLGTWAVLG-GOMYTPFNSA-N
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InChi Code |
InChI=1S/C23H30O4/c1-13-11-21-20-7-5-16-12-17(26)6-8-18(16)19(20)9-10-22(21,4)23(13,14(2)24)27-15(3)25/h12,18-21H,1,5-11H2,2-4H3/t18-,19+,20+,21-,22-,23-/m0/s1
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Chemical Name |
[(8R,9S,10R,13S,14S,17R)-17-acetyl-13-methyl-16-methylidene-3-oxo-2,6,7,8,9,10,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 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 (6.75 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 (6.75 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 | 2.6991 mL | 13.4956 mL | 26.9913 mL | |
5 mM | 0.5398 mL | 2.6991 mL | 5.3983 mL | |
10 mM | 0.2699 mL | 1.3496 mL | 2.6991 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 |
NCT04272008 | Completed | Drug: Segesterone Acetate and Ethinyl Estradiol Other: Tampon |
Contraception | TherapeuticsMD | March 6, 2020 | Phase 1 |
NCT04290390 | Completed | Drug: Segesterone Acetate and Ethinyl Estradiol Drug: Rifampin |
Women Hemodialysis |
TherapeuticsMD | February 12, 2020 | Phase 1 |