2. Anti-infection Metabolic Enzyme/Protease Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Fungal Cytochrome P450 Microtubule/Tubulin Mitochondrial Metabolism DNA/RNA Synthesis Apoptosis Fatty Acid Synthase (FASN)
  4. Prothioconazole

Prothioconazole is an orally active broad-spectrum fungicide. Prothioconazole weakly inhibits CaCYP51 activity in Candida albicans, with an apparent IC50 of approximately 120 μM. Prothioconazole disrupts Microtubule stability by reducing the acetylation level of α-tubulin. Prothioconazole induces Mitochondrial dysfunction, oxidative stress, DNA damage, and Apoptosis. Prothioconazole accumulates 14-methylated sterols and depletes ergosterol in cells, culture media, plants, and animals. Prothioconazole interferes with pyruvate metabolism and glycolysis/gluconeogenesis processes in mouse liver, downregulates Fasn mRNA expression, and induces hepatotoxicity and renal metabolic disorders. Prothioconazole reduces the fertility of female mice. Prothioconazole inhibits body weight gain and increases liver/kidney indices in mice. Prothioconazole can be used in studies related to candidiasis.

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Prothioconazole

Prothioconazole Chemical Structure

CAS No. : 178928-70-6

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

Other Forms of Prothioconazole:

Prothioconazole Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

View All DNA/RNA Synthesis Isoform Specific Products:

View All Isoforms
RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Prothioconazole is an orally active broad-spectrum fungicide. Prothioconazole weakly inhibits CaCYP51 activity in Candida albicans, with an apparent IC50 of approximately 120 μM. Prothioconazole disrupts Microtubule stability by reducing the acetylation level of α-tubulin. Prothioconazole induces Mitochondrial dysfunction, oxidative stress, DNA damage, and Apoptosis. Prothioconazole accumulates 14-methylated sterols and depletes ergosterol in cells, culture media, plants, and animals. Prothioconazole interferes with pyruvate metabolism and glycolysis/gluconeogenesis processes in mouse liver, downregulates Fasn mRNA expression, and induces hepatotoxicity and renal metabolic disorders. Prothioconazole reduces the fertility of female mice. Prothioconazole inhibits body weight gain and increases liver/kidney indices in mice. Prothioconazole can be used in studies related to candidiasis[1][2][3][4].

IC50 & Target[1]

CYP51

 

In Vitro

Prothioconazole shows weak binding affinity to purified *Candida albicans* CaCYP51, with an apparent dissociation constant Kd of 6.3 μM. It generates a type I difference spectrum instead of the typical type II difference spectrum produced by azole antifungal agents[1].
Prothioconazole (100 μM) competitively inhibits the binding of Lanosterol (HY-W020033) to purified *Candida albicans* CaCYP51, increasing the apparent Ks of Lanosterol by 2.5-fold to 62.2 μM[1].
Prothioconazole (0-100 μM) weakly inhibits CaCYP51 activity of Candida albicans in a cell-free system, with an apparent IC50 of approximately 120 μM, and only achieves an inhibition rate of 45% at a concentration of 100 μM[1].

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

Prothioconazole Related Antibodies
In Vivo

Prothioconazole (10 mg/kg/day; p.o.; daily; 30 days) exposure in female mice induces reproductive toxicity by disrupting oocyte maturation, fertilization, and early embryo development via mitochondrial dysfunction, oxidative stress, DNA damage, and apoptosis, reducing offspring numbers by ~34%[2].
Prothioconazole (1-5 mg/kg BW/day; p.o.; daily; 28 days) administration to male ICR mice causes dose-dependent oxidative stress, metabolic disruption, and reduced growth phenotypes, with more severe effects observed in liver tissue compared to kidney tissue[3].
Prothioconazole (1-5 mg/kg; p.o.; daily; 30 days) induces dose-dependent liver metabolic dysfunction and hepatotoxicity in female ICR mice, disrupting glycolipid metabolism via changes in key gene expression, metabolite levels, and liver histology[4].

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

Animal Model: ICR (female, 6-8-week-old)[2]
Dosage: 1 mg/kg/day; 5 mg/kg/day; 10 mg/kg/day
Administration: p.o.; daily; 30 days
Result: Reduced germinal vesicle breakdown (GVBD) rate to 75.3% (control: 89.5%).
Reduced first polar body extrusion (PBE) rate to 48.3% (control: 78.5%).
Reduced number of ovulated oocytes to 39.7 (control: 55.2).
Reduced fertilization rate to 78.5% (control: 95.9%).
Reduced 8-cell embryo rate to 52.6% (control: 63.8%).
Reduced morula rate to 35.1% (control: 61.2%).
Reduced blastocyst rate to 7.2% (control: 36.7%).
Reduced average offspring number to 10.1 (control: 15.3).
Increased aberrant spindle rate to 52.9% (control: 22.2%).
Increased misaligned chromosome rate to 28.6% (control: 15.9%).
Reduced acetylated α-tubulin fluorescence intensity to 15.4 A.U. (control: 32.2 A.U.).
Increased defective kinetochore-microtubule attachments rate to 46.1% (control: 14.3%).
Reduced Juno fluorescence intensity to 24.5 A.U. (control: 34.4 A.U.).
Reduced cortical granule fluorescence intensity to 28.7 A.U. (control: 40.7 A.U.).
Reduced ovastacin fluorescence intensity to 38.7 A.U. (control: 58.7 A.U.).
Reduced sperm binding number to 89.3 per egg (control: 143.8 per egg).
Reduced mitochondrial fluorescence intensity to 18.3 A.U. (control: 27.5 A.U.).
Increased ROS fluorescence intensity to 17.85 A.U. (control: 2.5 A.U.).
Increased γ-H2A.X fluorescence intensity to 21.5 A.U. (control: 13.4 A.U.).
Increased Annexin-V fluorescence intensity to 12.3 A.U. (control: 3.8 A.U.).
Identified 719 downregulated and 528 upregulated differentially expressed genes in oocytes, enriched in pathways related to mitochondrial oxidative phosphorylation, apoptosis, and oocyte meiosis.
Animal Model: ICR (5-week-old male)[3]
Dosage: 1 mg/kg BW/day; 5 mg/kg BW/day
Administration: p.o.; daily; 28 days
Result: Significantly decreased body weight gain and liver weight at both doses.
Significantly decreased liver index at 1 mg/kg dose; significantly decreased liver index, kidney weight, and kidney index at 5 mg/kg dose.
Did not significantly reduce body weight at either dose.
Significantly decreased glutathione (GSH) content in liver at both doses.
Significantly increased lipid peroxidation (LPO) content, superoxide dismutase (SOD) activity, and malondialdehyde (MDA) content in liver at 5 mg/kg dose; did not significantly increase LPO content in liver at 1 mg/kg dose.
Caused no significant changes to catalase (CAT) or peroxidase (POD) activity in liver at either dose.
Caused no significant changes to oxidative stress biomarkers in kidney at either dose.
Significantly increased relative abundances of lipid, lactate, acetate, choline, leucine, glutamate, glutamine, succinate, valine, alanine, lysine, and uracil in liver at both doses; significantly decreased relative abundances of phosphocholine (PC), glycerophosphocholine (GPC), and glycogen in liver at both doses.
Additionally significantly decreased relative abundances of alpha-glucose, beta-glucose, and betaine, and increased relative abundance of taurine in liver at 5 mg/kg dose.
Significantly decreased relative abundance of taurine in kidney at 1 mg/kg dose; significantly increased relative abundances of choline, PC, and glutamine, and decreased relative abundances of lactate, acetate, leucine, taurine, betaine, and succinate in kidney at 5 mg/kg dose.
Significantly altered D-glutamine and D-glutamate metabolism, alanine-aspartate-glutamate metabolism, pyruvate metabolism, and arginine biosynthesis in liver tissue at both doses.
Significantly altered phenylalanine, tyrosine, and tryptophan biosynthesis in kidney tissue at both doses; additionally significantly altered pyruvate metabolism, arginine biosynthesis, and taurine and hypotaurine metabolism in kidney tissue at 5 mg/kg dose.
Molecular Weight

344.26

Formula

C14H15Cl2N3OS
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

S=C1NC=NN1CC(CC2=C(Cl)C=CC=C2)(C3(CC3)Cl)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (145.24 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 2.9048 mL 14.5239 mL 29.0478 mL
5 mM 0.5810 mL 2.9048 mL 5.8096 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (7.26 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 (7.26 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
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: 99.52%

SDS (761 KB)

COA (252 KB)

Handling Instructions (2659 KB)
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 2.9048 mL 14.5239 mL 29.0478 mL 72.6195 mL
5 mM 0.5810 mL 2.9048 mL 5.8096 mL 14.5239 mL
10 mM 0.2905 mL 1.4524 mL 2.9048 mL 7.2620 mL
15 mM 0.1937 mL 0.9683 mL 1.9365 mL 4.8413 mL
20 mM 0.1452 mL 0.7262 mL 1.4524 mL 3.6310 mL
25 mM 0.1162 mL 0.5810 mL 1.1619 mL 2.9048 mL
30 mM 0.0968 mL 0.4841 mL 0.9683 mL 2.4207 mL
40 mM 0.0726 mL 0.3631 mL 0.7262 mL 1.8155 mL
50 mM 0.0581 mL 0.2905 mL 0.5810 mL 1.4524 mL
60 mM 0.0484 mL 0.2421 mL 0.4841 mL 1.2103 mL
80 mM 0.0363 mL 0.1815 mL 0.3631 mL 0.9077 mL
100 mM 0.0290 mL 0.1452 mL 0.2905 mL 0.7262 mL
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Prothioconazole Related Classifications

Help & FAQs
  • 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.

Keywords:

Prothioconazole178928-70-6JAU-6476JAU6476JAU 6476FungalCytochrome P450Microtubule/TubulinMitochondrial MetabolismDNA/RNA SynthesisApoptosisFatty Acid Synthase (FASN)CYPsMycosphaerella graminicola CYP51candidiasismitochondrial dysfunctionCandida albicans ATCC SC5314ICR miceprothioconazole-desthioCaCYP51ergosterolα-tubulinCandida albicansInhibitorinhibitorinhibit

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