1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. Endogenous Metabolite Estrogen Receptor/ERR
  3. Estrone sulfate potassium

Estrone sulfate potassium is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate potassium is also a substrate of the OATP1B3 transporter. Estrone sulfate potassium can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate potassium stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate potassium is applicable to breast cancer-related research.

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Estrone sulfate potassium

Estrone sulfate potassium Chemical Structure

CAS No. : 1240-04-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 3 publication(s) in Google Scholar

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Description

Estrone sulfate potassium is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate potassium is also a substrate of the OATP1B3 transporter. Estrone sulfate potassium can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate potassium stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate potassium is applicable to breast cancer-related research[1][2][3][4].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Estrone sulfate (1.0 μM; 1-64 min) potassium is taken up at a low rate by dispersed normal breast parenchymal cells, resulting in a cells/medium concentration ratio of 0.20-0.33 when incubated at 37°C[2].
Estrone sulfate (1.0 nM-100 μM) potassium is converted to estrone by dispersed normal breast parenchymal cells with a mean half-time of 628 min per 106 cells (intact cells) or 246 min per 106 cells (homogenized cells)[2].
Estrone sulfate potassium is not produced via conversion of estrone by dispersed normal breast parenchymal cells under conditions where MCF-7 breast cancer cells exhibit sulfotransferase activity[2].
Estrone sulfate potassium stimulates colony formation in dispersed nitrosomethylurea mammary cells and is converted to estrone and estradiol by these cells[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Estrone sulfate (30-3000 pmol/hr; 400-1300 pmol/hr; s.c.; continuous infusion; 14 days) potassium exerts dose-related stimulatory effects on nitrosomethylurea-induced hormone-responsive mammary tumor growth in castrate rats, with significant conversion to estrone and estradiol[3].
Estrone sulfate (75 mg/kg; p.o; daily; for 5 days) potassium reduces glucose-6-phosphatase activity and protein levels, and lowers blood glucose in ob/ob mice[4].
Estrone sulfate potassium modulates glucose-6-phosphatase kinetic parameters in control mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (female, castrated, nitrosomethylurea-induced mammary tumor model)[3]
Dosage: 30 pmol/hr; 300 pmol/hr; 3000 pmol/hr; 400 pmol/hr; 1300 pmol/hr
Administration: s.c.; continuous infusion; 14 days
Result: Did not significantly alter castration-induced tumor regression at 30 pmol/hr; partially blunted castration-induced tumor regression at 300 pmol/hr; stimulated tumor growth at 3000 pmol/hr; Observed significantly different tumor growth slopes for 300 and 3000 pmol/hr doses; Detected 14%, 10%, and 13% conversion to estradiol, and 24%, 22%, and 28% conversion to estrone on days 7, 10, and 14, respectively, at 400 pmol/hr; Recorded similar conversion rates at 1300 pmol/hr; Measured serum estradiol levels of 17 pg/ml (400 pmol/hr), 56 pg/ml (1300 pmol/hr), 6.8 ± 1.2 pg/ml (300 pmol/hr, day 14), and 48 ± 10.2 pg/ml (3000 pmol/hr, day 14).
Molecular Weight

388.52

Formula

C18H21KO5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]1([C@](CC2)([H])[C@]3([H])CCC4=C(C=CC(OS(=O)([O-])=O)=C4)[C@@]3([H])CC1)C2=O.[K+]

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (257.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5739 mL 12.8694 mL 25.7387 mL
5 mM 0.5148 mL 2.5739 mL 5.1477 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.94%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5739 mL 12.8694 mL 25.7387 mL 64.3468 mL
5 mM 0.5148 mL 2.5739 mL 5.1477 mL 12.8694 mL
10 mM 0.2574 mL 1.2869 mL 2.5739 mL 6.4347 mL
15 mM 0.1716 mL 0.8580 mL 1.7159 mL 4.2898 mL
20 mM 0.1287 mL 0.6435 mL 1.2869 mL 3.2173 mL
25 mM 0.1030 mL 0.5148 mL 1.0295 mL 2.5739 mL
30 mM 0.0858 mL 0.4290 mL 0.8580 mL 2.1449 mL
40 mM 0.0643 mL 0.3217 mL 0.6435 mL 1.6087 mL
50 mM 0.0515 mL 0.2574 mL 0.5148 mL 1.2869 mL
60 mM 0.0429 mL 0.2145 mL 0.4290 mL 1.0724 mL
80 mM 0.0322 mL 0.1609 mL 0.3217 mL 0.8043 mL
100 mM 0.0257 mL 0.1287 mL 0.2574 mL 0.6435 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Estrone sulfate potassium
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HY-113293A
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