| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Estropipate is an estrogen receptor agonist. After administration, estropipate is converted in vivo to active estrogens, including estrone and estradiol, which bind estrogen receptors and regulate gene expression. Estropipate is also a potent, selective inhibitor of organic anion transporting polypeptides 1B1 (OATP1B1) with an IC₅₀ of 0.05 µM for human OATP1B1.
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| ln Vitro |
In vitro, estropipate is an estrogen receptor agonist. It is a potent inhibitor of OATP1B1 with an IC₅₀ of 0.05 µM for human OATP1B1 and 0.12 µM for cynomolgus monkey OATP1B1. Its activity can be assessed using estrogen receptor binding assays, cell-based reporter gene assays, and OATP1B1 transport assays.
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| ln Vivo |
In vivo, estropipate is used for hormone replacement therapy to alleviate menopausal symptoms and to prevent osteoporosis in high-risk populations. It is converted in vivo to active estrogens, including estrone and estradiol. Estropipate has been used clinically for these indications.
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| Enzyme Assay |
Non-cellular receptor binding assays for estropipate involve competitive radioligand binding displacement studies using estrogen receptor preparations. The receptor is incubated with a radiolabeled estradiol ligand and varying concentrations of estropipate. Following incubation and filtration, bound radioactivity is measured. IC₅₀ values are determined from displacement curves. OATP1B1 inhibition can be assessed using membrane vesicle transport assays.
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| Cell Assay |
In vitro cellular assays for estropipate involve treating cells expressing estrogen receptors with the compound and measuring receptor-mediated transcriptional activity. Reporter gene assays using estrogen response element (ERE)-luciferase constructs are commonly used. OATP1B1 inhibition is assessed using cells expressing OATP1B1 and a fluorescent or radiolabeled substrate. The inhibition of substrate uptake is quantified.
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| Animal Protocol |
In vivo animal experiments with estropipate are conducted in ovariectomized rat models of menopause. Rats are treated with estropipate via oral administration, and effects on bone density (measured by DEXA), uterine weight, and vaginal epithelium are assessed. The compound's ability to prevent bone loss and alleviate menopausal symptoms is evaluated.
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| ADME/Pharmacokinetics |
Estropipate has a molecular weight of 436.56 and a molecular formula of C₁₈H₂₂O₅S·C₄H₁₀N₂. It is a solid powder with a purity of ≥97%. The compound is typically stored at room temperature. It is soluble in DMSO and other organic solvents. The compound is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Estropipate is generally well-tolerated at therapeutic doses. As a hormone replacement therapy, it may cause side effects similar to other estrogens, including breast tenderness, nausea, and increased risk of thromboembolic events. It should be used with caution in patients with a history of thromboembolic disorders, breast cancer, or liver disease.
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| References |
Bagdade JD, Subbaiah PV. Effects of estropipate treatment on plasma lipids and
lipoprotein lipid composition in postmenopausal women. J Clin Endocrinol Metab.
1991 Feb;72(2):283-6. PubMed PMID: 1991799.
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| Additional Infomation |
According to state or federal labeling requirements, estronepiperidine may be carcinogenic and developmentally toxic. Estronepiperidine is a steroid sulfate and piperazine salt. It is functionally related to estrone. Estronepiperidine is a natural estrogenic substance composed of estrone sulfate and piperazine. Estronepiperidine diffuses across cell membranes and binds to nuclear estrogen receptors present in the reproductive tract, mammary glands, pituitary gland, hypothalamus, liver, and bones, thereby activating these receptors. The activated complex binds to estrogen-responsive elements on DNA, activating the transcription of genes involved in female reproductive system function and secondary sexual characteristic development. See also: Estrone (with active moiety).
Estropipate (Piperazine Estrone Sulfate; CAS 7280-37-7) is an estrogen receptor agonist used in hormone replacement therapy for menopausal symptoms and osteoporosis prevention. It is converted in vivo to active estrogens, including estrone and estradiol. Estropipate is also a potent inhibitor of OATP1B1 with an IC₅₀ of 0.05 µM. The compound is available from various commercial suppliers for research applications. |
| Molecular Formula |
C22H32N2O5S
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|---|---|
| Molecular Weight |
436.5649
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| Exact Mass |
436.203
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| Elemental Analysis |
C, 60.53; H, 7.39; N, 6.42; O, 18.32; S, 7.34
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| CAS # |
7280-37-7
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| Related CAS # |
7280-37-7
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| PubChem CID |
5284555
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| Appearance |
White to off-white solid powder
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| LogP |
4.211
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
650
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S(=O)(=O)(O[H])OC1C([H])=C([H])C2=C(C=1[H])C([H])([H])C([H])([H])[C@]1([H])[C@]2([H])C([H])([H])C([H])([H])[C@]2(C([H])([H])[H])C(C([H])([H])C([H])([H])[C@]21[H])=O.N1([H])C([H])([H])C([H])([H])N([H])C([H])([H])C1([H])[H]
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| InChi Key |
HZEQBCVBILBTEP-ZFINNJDLSA-N
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| InChi Code |
InChI=1S/C18H22O5S.C4H10N2/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19;1-2-6-4-3-5-1/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22);5-6H,1-4H2/t14-,15-,16+,18+;/m1./s1
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| Chemical Name |
[(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate;piperazine
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| Synonyms |
Estropipate; Piperazine estrone sulfate; Piperazine estronesulfate; Harmogen; Ogen
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 87~110 mg/mL (199.3~252 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.30 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 27.5 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: ≥ 2.75 mg/mL (6.30 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 27.5 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: ≥ 2.75 mg/mL (6.30 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 | 2.2906 mL | 11.4532 mL | 22.9064 mL | |
| 5 mM | 0.4581 mL | 2.2906 mL | 4.5813 mL | |
| 10 mM | 0.2291 mL | 1.1453 mL | 2.2906 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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