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| Other Sizes |
Purity: ≥98%
| Targets |
Metabolite; ER; steroid hormone
Estradiol dipropionate targets estrogen receptors (ERα and ERβ) in various tissues throughout the body. After administration, the compound is hydrolyzed to estradiol, which binds to and activates estrogen receptors. This activation regulates the transcription of estrogen-responsive genes, leading to the physiological effects of estrogen, including the development and maintenance of female reproductive tissues, regulation of the menstrual cycle, and maintenance of bone density. |
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| ln Vitro |
Ovariectomized mice had reduced levels of β-catenin and GSK-3β in their luminal and glandular epithelia after receiving treatment with estradiol dipropionate (2μg per 100 g; single subcutaneous injection) and chorionic gonadotropin (10 IU per 100 g; sc; twice a day) for two days[1].
The incidence of atypical endometrial hyperplasia is significantly higher, the level of β-catenin is slightly higher, and the expression of GSK-3β is lower in luminal and glandular epithelia after treatment with estradiol dipropionate (2 μg per 100 g; once a week) and chorionic gonadotropin (10 IU per 100 g; once a day) for a month[1]. In vitro, Estradiol dipropionate is hydrolyzed to estradiol in cell culture systems. The released estradiol binds to estrogen receptors and activates estrogen-responsive gene expression. Estradiol dipropionate and its metabolite estradiol have been shown to promote the proliferation of estrogen receptor-positive breast cancer cell lines. They also modulate the expression of various genes involved in cell cycle regulation, apoptosis, and differentiation. |
| ln Vivo |
β-catenin and GSK in luminal and glandular epithelium following 2 days of treatment with estradiol dipropionate (2 μg/100 g; single subcutaneous injection) and chorionic gonadotropin (10 IU/100 g; subcutaneous injection; twice daily) Levels of -3β are lower in ovariectomized animals [1]. After one month of treatment with estradiol dipropionate (2μg/100g; once a week) and chorionic gonadotropin (10IU/100g; once a day), the incidence of atypical endometrial hyperplasia was dramatically raised, and the level of β-catenin rose. The expression of GSK-3β is slightly higher in high luminal epithelium and glandular epithelium, while the expression of GSK-3β is lower [1].
In vivo, Estradiol dipropionate produces estrogenic effects after administration. It is used in hormone replacement therapy to alleviate menopausal symptoms such as hot flashes, vaginal dryness, and mood swings. Estradiol dipropionate also helps to prevent osteoporosis by maintaining bone density. The compound has been shown to have beneficial effects on cardiovascular health and cognitive function in postmenopausal women. |
| Enzyme Assay |
In vitro assays for Estradiol dipropionate typically involve measuring its hydrolysis to estradiol in cell culture or in the presence of esterases. The binding affinity of the released estradiol to estrogen receptors can be assessed using receptor binding assays. Estrogen-responsive reporter gene assays can be used to measure the transcriptional activity of the compound. The proliferation of estrogen receptor-positive breast cancer cells can be used as a bioassay for estrogenic activity.
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| Cell Assay |
In vitro cell-based studies with Estradiol dipropionate typically involve culturing estrogen receptor-positive cell lines such as MCF-7 or T47D cells. Cells are treated with Estradiol dipropionate at various concentrations, and cell proliferation is measured using MTT or similar assays. Estrogen-responsive gene expression is measured by quantitative PCR or Western blot analysis. The effect of the compound on cell cycle progression and apoptosis can also be evaluated.
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| Animal Protocol |
This work examined the effect of chorionic gonadotropin on proliferative and morphogenetic reactions in the uterus under short- and long-term estrogen treatments. Ovariectomized mice received a single injection with estradiol dipropionate (2 micro g per 100 g; subcutaneously, sc) or vehicle and injections with human chorionic gonadotropin (10 IU per 100 g; sc) or vehicle twice a day for 2 days. Other groups of animals received injections with estradiol once a week or vehicle and injections with chorionic gonadotropin or vehicle once a day for 30 days. The uteri were removed 48 h after the last estradiol or vehicle injection. In animals treated with estradiol and chorionic gonadotropin for a month, the incidence of atypical endometrial hyperplasia was significantly higher. In animals treated with estradiol and chorionic gonadotropin for 2 days or for a month, uterine mass was slightly increased, the number of mitotic cells and BrdU-labeled cells was greater in luminal epithelium, glandular epithelium, stromal and myometrial cells, whereas the expression of estrogen receptors-alpha was lower in all uterine compartments, than in control. In mice who received estradiol and chorionic gonadotropin for 2 days, levels of beta-catenin and glycogen synthase kinase-3beta in luminal and glandular epithelia were lower. In animals treated with estradiol and chorionic gonadotropin for a month, the level of beta-catenin was slightly higher, and the expression of glycogen synthase kinase-3beta was lower in luminal and glandular epithelia. Thus, chorionic gonadotropin exerts estradiol-induced proliferative and morphogenetic changes in the uterus. This action of chorionic gonadotropin is associated with decreased expression of estrogen receptors-alpha and with changes in expression of beta-catenin and glycogen synthase kinase-3beta in the uterus.[1]
In vivo animal studies with Estradiol dipropionate are typically conducted in ovariectomized rodent models, which mimic the estrogen-deficient state of postmenopausal women. The compound is administered by injection, and its effects on uterine weight, bone density, and vaginal epithelium are assessed. The compound's ability to alleviate menopausal symptoms is evaluated. Pharmacokinetic studies are performed to measure estradiol levels in plasma. |
| ADME/Pharmacokinetics |
Estradiol dipropionate is a prodrug with well-characterized pharmacokinetic properties. Following injection, it is slowly absorbed from the injection site and hydrolyzed to estradiol. Estradiol is then distributed to various tissues. Estradiol is metabolized in the liver, primarily by cytochrome P450 enzymes, to estrone and other metabolites. The metabolites are excreted in the urine. The half-life of estradiol dipropionate is longer than that of estradiol due to the sustained release from the injection site.
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| Toxicity/Toxicokinetics |
Estradiol dipropionate is a clinically approved hormone therapy with a well-established safety profile. The most common adverse effects are related to estrogenic effects and include breast tenderness, nausea, headache, and fluid retention. Long-term use of estrogen therapy has been associated with an increased risk of breast cancer, endometrial cancer, and thromboembolic events. The risks and benefits of hormone therapy should be carefully evaluated for each patient.
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| References | |
| Additional Infomation |
Estradiol dipropionate is a steroidal ester. It is the synthetic dipropionate of estradiol, a steroidal sex hormone essential for maintaining female fertility and secondary sexual characteristics. As the primary and most potent estrogen produced by the ovaries, estradiol binds to and activates specific nuclear receptors. This drug has mild anabolic and metabolic effects and can enhance blood clotting. (NCI04)
Estradiol dipropionate is a clinically approved estrogen used in hormone replacement therapy. It is available in various formulations for injection. Estradiol dipropionate is used for the treatment of menopausal symptoms, estrogen deficiency, and in some cases, for the palliative treatment of breast cancer. The compound is available under various brand names. It is a Schedule III controlled substance in some jurisdictions. |
| Molecular Formula |
C24H32O4
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|---|---|
| Molecular Weight |
384.52
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| Exact Mass |
384.23
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| Elemental Analysis |
C, 74.97; H, 8.39; O, 16.64
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| CAS # |
113-38-2
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| Related CAS # |
113-38-2; Alpha-Estradiol;57-91-0;Estradiol (Standard);50-28-2;Estradiol-d3;79037-37-9;Estradiol-d4;66789-03-5;Estradiol-d5;221093-45-4;Estradiol-13C2;82938-05-4;Estradiol (cypionate);313-06-4;Estradiol benzoate;50-50-0;Estradiol enanthate;4956-37-0;Estradiol hemihydrate;35380-71-3;Estradiol-d2;53866-33-4;Estradiol-13C6;Estradiol-d2-1;3188-46-3;rel-Estradiol-13C6; 979-32-8 (valerate); 113-38-2 (dipropionate); 57-63-6 (ethinyl); 172377-52-5 (sulfamate); 3571-53-7 (undecylate)
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| PubChem CID |
8225
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| Appearance |
White to off-white solid powder
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| Density |
1.14g/cm3
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| Boiling Point |
487.8ºC at 760mmHg
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| Melting Point |
104-106℃ (ethanol )
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| Flash Point |
238.5ºC
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| Vapour Pressure |
3.58E-09mmHg at 25°C
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| Index of Refraction |
1.577
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| LogP |
5.179
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
601
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O(C(C([H])([H])C([H])([H])[H])=O)[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4C([H])=C(C([H])=C([H])C=4[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])OC(C([H])([H])C([H])([H])[H])=O
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| InChi Key |
JQIYNMYZKRGDFK-RUFWAXPRSA-N
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| InChi Code |
InChI=1S/C24H32O4/c1-4-22(25)27-16-7-9-17-15(14-16)6-8-19-18(17)12-13-24(3)20(19)10-11-21(24)28-23(26)5-2/h7,9,14,18-21H,4-6,8,10-13H2,1-3H3/t18-,19-,20+,21+,24+/m1/s1
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| Chemical Name |
[(8R,9S,13S,14S,17S)-13-methyl-3-propanoyloxy-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] propanoate
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| Synonyms |
Estradiol dipropionate; Estronex; Diprostron; Diovocylin; Agofollin; Progynon-DP; Dimenformon dipropionate; Diovocyclin; Follicyclin P; Estroici
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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: 21~62.5 mg/mL (54.6~162.5 mM)
Ethanol: ~20 mg/m L(~52.0 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 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 20.8 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: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6006 mL | 13.0032 mL | 26.0064 mL | |
| 5 mM | 0.5201 mL | 2.6006 mL | 5.2013 mL | |
| 10 mM | 0.2601 mL | 1.3003 mL | 2.6006 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.
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