| 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 |
| Targets |
Promestriene targets estrogen receptors (ERs) within target cells. By binding to and activating these intracellular estrogen receptors, it exerts estrogenic effects on the vaginal mucosa, alleviating symptoms such as vaginal dryness and itching. Its design minimizes systemic absorption, thus limiting its effects primarily to the local site of application.
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| ln Vitro |
Gynecological creams or capsules containing proestrenol, an estradiol analogue, can be injected intravaginally without causing systemic effects or limited absorption [2]. Topical proestren is barely absorbed when used consistently, and studies have shown that it greatly reduces vaginal atrophy symptoms [3].
In vitro, promestriene is an analogue of oestradiol. As a locally effective estrogen, its activity is assessed by its ability to bind to and activate estrogen receptors in target cells. It is used to investigate therapeutic interventions for conditions associated with estrogen deficiency. |
| ln Vivo |
In vivo, promestriene has an efficient action on vaginal atrophy while being minimally absorbed. After vaginal administration, it acts on the vaginal mucosa to alleviate atrophy and related symptoms. Its minimal systemic absorption reduces the risk of systemic side effects associated with estrogen therapy.
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| Enzyme Assay |
Non-cellular assays for promestriene involve measuring its binding affinity to estrogen receptors (ERα and ERβ). This is typically done using competitive binding assays with a radiolabeled estradiol ligand. The compound's ability to displace the radioligand is used to calculate its relative binding affinity.
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| Cell Assay |
In vitro cellular assays for promestriene are conducted in cells expressing estrogen receptors, such as MCF-7 breast cancer cells. The compound's ability to activate ER-mediated transcription is measured using a luciferase reporter gene under the control of an estrogen-responsive element (ERE). Its proliferative effects on ER-positive cells can also be assessed.
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| Animal Protocol |
In vivo animal experiments with promestriene are conducted in ovariectomized rat or mouse models, which mimic post-menopausal estrogen deficiency. The compound is administered vaginally or topically, and its effects on vaginal epithelial thickness, lubrication, and histological changes are assessed. Systemic absorption and uterine weight (a marker of systemic estrogenic activity) are also measured to confirm its localized action.
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| ADME/Pharmacokinetics |
Promestriene is minimally absorbed after topical or vaginal administration. This local action allows for higher concentrations in the target tissue while minimizing systemic exposure and side effects. The compound is typically stored at room temperature.
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| Toxicity/Toxicokinetics |
Promestriene is generally well-tolerated when used topically. Due to its minimal systemic absorption, systemic side effects are rare. Local irritation may occur. It is contraindicated in patients with known hypersensitivity to the drug or in those with estrogen-dependent malignancies. It is not approved for systemic use.
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| References |
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| Additional Infomation |
Promestriene is a steroid derived from the hydrogenation of estradiol. Promestriene (3-propylethyl-17β-methylestradiol) has been used in clinical trials for the prevention of hypospadias. It is a synthetic estrogen analog used for topical estrogen therapy. If the extremely low absorption rate of promestriene results in estrogen-like effects on cell proliferation and estrogen-responsive gene expression, its potential to treat aromatase inhibitor-related vaginal atrophy symptoms will not be realized. There are concerns that vaginally absorbed estrogens or estrogen analogs may activate occult residual breast cancer lesions or counteract the tumor-suppressive effects of aromatase inhibitor adjuvant therapy. Promestriene has been investigated in a phase IV clinical trial for its effects on improving hormonal cytology, local and systemic menopausal symptoms, and endometrial safety in patients with atrophic pelvic vaginitis, organ prolapse, and endometrial hyperplasia. It has also been investigated in a phase III clinical trial for its efficacy in patients after hypospadias surgery. In addition, Promestriene underwent a Phase IV clinical trial to investigate its therapeutic effects on patients with bacterial vaginosis, but this study has been terminated. Promestriene is the 3-propyl and 17β-methyl ether of estradiol and can be administered vaginally to relieve vaginal atrophy and related symptoms. After vaginal administration, Promestriene acts on the vaginal mucosa to alleviate vaginal atrophy and related symptoms such as vaginal dryness and itching.
Promestriene is a synthetic, locally effective estrogen used to treat vaginal atrophy. It is a diethyl-ether of estradiol designed for minimal systemic absorption. It is available as a topical cream and is used in research for conditions associated with estrogen deficiency. |
| Molecular Formula |
C22H32O2
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|---|---|
| Molecular Weight |
328.4883
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| Exact Mass |
328.24
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| CAS # |
39219-28-8
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| PubChem CID |
9883915
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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 |
436.8±45.0 °C at 760 mmHg
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| Melting Point |
64-660ºC
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| Flash Point |
153.3±28.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.546
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| LogP |
6.48
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
436
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CCCOC1=CC2=C(C=C1)[C@H]3CC[C@]4([C@H]([C@@H]3CC2)CC[C@@H]4OC)C
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| InChi Key |
IUWKNLFTJBHTSD-AANPDWTMSA-N
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| InChi Code |
InChI=1S/C22H32O2/c1-4-13-24-16-6-8-17-15(14-16)5-7-19-18(17)11-12-22(2)20(19)9-10-21(22)23-3/h6,8,14,18-21H,4-5,7,9-13H2,1-3H3/t18-,19-,20+,21+,22+/m1/s1
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| Chemical Name |
(8R,9S,13S,14S,17S)-17-methoxy-13-methyl-3-propoxy-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene
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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 : ~20 mg/mL (~60.88 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (6.09 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 20.0 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 mg/mL (6.09 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 20.0 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 | 3.0442 mL | 15.2212 mL | 30.4423 mL | |
| 5 mM | 0.6088 mL | 3.0442 mL | 6.0885 mL | |
| 10 mM | 0.3044 mL | 1.5221 mL | 3.0442 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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