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Sulfathiazole is an orally active, endocrine disruptor targeting the steroidogenic pathway, specifically enhancing the activity of CYP19 in human adrenal cancer cells (H295R) and upregulating the mRN expression of CYP17, CYP19, and 3β-HSD. Sulfathiazole increases the production of 17-estradiol (E2) and has endocrine disrupting effects on aquatic organisms such as the Japanese medaka fish.

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Sulfathiazole

Sulfathiazole Chemical Structure

CAS No. : 72-14-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 5 publication(s) in Google Scholar

Other Forms of Sulfathiazole:

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  • Purity & Documentation

  • References

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Description

Sulfathiazole is an orally active, endocrine disruptor targeting the steroidogenic pathway, specifically enhancing the activity of CYP19 in human adrenal cancer cells (H295R) and upregulating the mRN expression of CYP17, CYP19, and 3β-HSD. Sulfathiazole increases the production of 17-estradiol (E2) and has endocrine disrupting effects on aquatic organisms such as the Japanese medaka fish[1][2][3].

IC50 & Target

Antibacterial

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
4161 μM
Compound: 3a
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay
[PMID: 22365879]
Sf9 IC50
430 μM
Compound: 19
Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
Inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay
[PMID: 26824386]
In Vitro

Sulfathiazole (0.02-20 mg/L; 48 h) can significantly increase the production of 17-estradiol (E2), aromatase (CYP19) activity, and mRNA expression of steroidogenesis-related genes such as CYP17, CYP19, and 3βHSD in human adrenal cancer cell (H295R) experiments[1].
Sulfathiazole can effectively inhibit the corrosion of copper in 0.1 M NaCl solution, and the inhibition efficiency can reach more than 80% with increasing concentration[3].

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

Cell Viability Assay[1]

Cell Line: H295R cells
Concentration: 0.2 mg/L, 2 mg/L
Incubation Time: 48 h
Result: Exposure to 0.2 mg/L and 2 mg/L Sulfathiazole for 48 h upregulated the mRNA expression of CYP17, CYP19, and 3βHSD2, which are key genes involved in the steroidogenic pathway.
In Vivo

Sulfathiazole (50 mg/L, 500 mg/L; water exposure; daily feeding; 14 days) significantly increases plasma 17-estradiol (E2) concentrations in male Japanese medaka (Oryzias latipes) models[1].
Sulfathiazole (1%; mixed in purified feed; daily intake) causes a decrease in polymorphonuclear neutrophils, band cells, and metamyelocytes in the bone marrow, necrosis and calcification of skeletal muscle, calcification or hyalinization of pulmonary/coronary/renal arteries, hydropic degeneration and focal hyaline necrosis of hepatocytes, hyaline necrosis of adrenal cortical cells, thyroid hyperplasia, and hemorrhage in subcutaneous tissues, body cavities, and organs in Wistar and Osborne-Mendel albino rat models during and shortly after weaning[2].

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

Animal Model: Male Japanese medaka (Oryzias latipes), 3-4 months old[1]
Dosage: 50 mg/L, 500 mg/L (water)
Administration: Waterborne exposure with ad libitum feeding of Artemia nauplii twice daily, renewed exposure medium at least three times per week for 14 d
Result: After 14-d exposure, plasma E2 concentrations in male medaka were significantly increased to 1.56 ng/mL (50 mg/L) and 2.06 ng/mL (500 mg/L), which were 1.32-fold and 1.75-fold higher than the control (1.18 ng/mL), respectively.
Molecular Weight

255.32

Formula

C9H9N3O2S2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N)C=C1)(NC2=NC=CS2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (783.33 mM; ultrasonic and warming and heat to 60°C; 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 3.9167 mL 19.5833 mL 39.1665 mL
5 mM 0.7833 mL 3.9167 mL 7.8333 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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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: ≥ 5 mg/mL (19.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (19.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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:
%
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+
%
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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).
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: 99.95%

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. 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 3.9167 mL 19.5833 mL 39.1665 mL 97.9163 mL
5 mM 0.7833 mL 3.9167 mL 7.8333 mL 19.5833 mL
10 mM 0.3917 mL 1.9583 mL 3.9167 mL 9.7916 mL
15 mM 0.2611 mL 1.3056 mL 2.6111 mL 6.5278 mL
20 mM 0.1958 mL 0.9792 mL 1.9583 mL 4.8958 mL
25 mM 0.1567 mL 0.7833 mL 1.5667 mL 3.9167 mL
30 mM 0.1306 mL 0.6528 mL 1.3056 mL 3.2639 mL
40 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4479 mL
50 mM 0.0783 mL 0.3917 mL 0.7833 mL 1.9583 mL
60 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6319 mL
80 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL
100 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9792 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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Sulfathiazole
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