2. Stem Cell/Wnt TGF-beta/Smad NF-κB
  3. TGF-beta/Smad NF-κB
  4. (Rac)-Hesperetin

(Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects.

For research use only. We do not sell to patients.

(Rac)-Hesperetin

(Rac)-Hesperetin Chemical Structure

CAS No. : 69097-99-0

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

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(Rac)-Hesperetin Related Antibodies

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Description

(Rac)-Hesperetin is the racemate of Hesperetin (HY-N0168), an orally active multi-target inhibitor. (Rac)-Hesperetin exhibits significant anti-tumor and anti-inflammatory activities by blocking the TGF-β1-mediated Fyn/RhoA signaling axis and the TLR4-MyD88-NF-κB inflammatory pathway. (Rac)-Hesperetin inhibits the formation of actin stress fibers and the migration and invasion of cancer cells, and is suitable for triple-negative breast cancer research. In inflammation models, (Rac)-Hesperetin effectively alleviates lung injury by reducing the release of pro-inflammatory mediators and regulating the activity of oxidative stress enzymes, and is suitable for acute lung injury research. (Rac)-Hesperetin also interferes with the entry and early replication processes of channel catfish virus, inhibits viral gene expression and progeny virus production, thereby protecting cells from virus-induced cytopathic effects[1][2][3].

In Vitro

Hesperetin (25, 50, 100 μM; 0, 24, 48, 72 h) significantly inhibits the migratory capacity of TGF-β1-induced human triple-negative breast cancer MDA-MB-231 cells in a dose-dependent manner[1].
Hesperetin (500 μg/mL; 36 h) significantly inhibits the expression of ORF39 and ORF59 proteins of CCV, completely alleviates the cytopathic effect on CCO cells induced by CCV infection, and exerts a cytoprotective effect[2].

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

(Rac)-Hesperetin Related Antibodies

Cell Viability Assay[1]

Cell Line: Human triple-negative breast cancer MDA-MB-231 cells
Concentration: 25, 50, 100 μM
Incubation Time: 24, 48, 72 h
Result: Significantly inhibited TGF-β1-induced migration of MDA-MB-231 cells in a dose-dependent manner at 24 h, 48 h and 72 h after treatment.
In Vivo

Hesperetin (10-30 mg/kg; intragastric administration; single dose; administered 1 h after lipopolysaccharide modeling) significantly reduces the levels of IL-6 and TNF-α as well as the number of inflammatory cells in bronchoalveolar lavage fluid, alleviates lung tissue injury, decreases the lung wet/dry weight ratio, downregulates the activities of myeloperoxidase and lactate dehydrogenase, and enhances the activity of superoxide dismutase in a lipopolysaccharide-induced acute lung injury model of male C57 mice[3].

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

Animal Model: C57 male mice (8 weeks old, 18-22 g) with LPS-induced acute lung injury[3]
Dosage: Hesperetin: 10 mg/kg, 20 mg/kg , 30 mg/kg ;
Positive control: 2 mg/kg Dexamethasone (oral gavage)
Administration: oral gavage
Result: At 1 h after LPS intratracheal instillation, significantly suppressed the levels of interleukin-6 and tumor necrosis factor-α in bronchoalveolar lavage fluid, reduced the number of inflammatory cells in bronchoalveolar lavage fluid, ameliorated LPS-induced histopathologic changes of lung tissue and decreased lung inflammatory scores.
Reduced the lung wet/dry weight ratio, lowered the activities of myeloperoxidase and lactate dehydrogenase in lung tissue, enhanced superoxide dismutase activity, and downregulated the protein expression of Toll-like receptor 4 and myeloid differentiation factor 88 in lung tissue.
Suppressed the phosphorylation of nuclear factor-κB p65, IκB-α and TAK1, and inhibited the activation of nuclear factor-κB pathway in lung tissue, with the 30 mg/kg dosage showing the most significant therapeutic effect.
Molecular Weight

302.28

Formula

C16H14O6
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1CC(C2=CC=C(OC)C(O)=C2)OC3=CC(O)=CC(O)=C13
Structure Classification
Initial Source
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 : 125 mg/mL (413.52 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 3.3082 mL 16.5410 mL 33.0819 mL
5 mM 0.6616 mL 3.3082 mL 6.6164 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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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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 +
% 
+
%
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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: 99.28%

SDS (393 KB)

COA (248 KB) LCMS (88 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 3.3082 mL 16.5410 mL 33.0819 mL 82.7048 mL
5 mM 0.6616 mL 3.3082 mL 6.6164 mL 16.5410 mL
10 mM 0.3308 mL 1.6541 mL 3.3082 mL 8.2705 mL
15 mM 0.2205 mL 1.1027 mL 2.2055 mL 5.5137 mL
20 mM 0.1654 mL 0.8270 mL 1.6541 mL 4.1352 mL
25 mM 0.1323 mL 0.6616 mL 1.3233 mL 3.3082 mL
30 mM 0.1103 mL 0.5514 mL 1.1027 mL 2.7568 mL
40 mM 0.0827 mL 0.4135 mL 0.8270 mL 2.0676 mL
50 mM 0.0662 mL 0.3308 mL 0.6616 mL 1.6541 mL
60 mM 0.0551 mL 0.2757 mL 0.5514 mL 1.3784 mL
80 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
100 mM 0.0331 mL 0.1654 mL 0.3308 mL 0.8270 mL
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(Rac)-Hesperetin 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:

(Rac)-Hesperetin69097-99-0TGF-beta/SmadNF-κBTransforming growth factor betaNuclear factor-κBNuclear factor-kappaBRho-kinaseTGF-β1TLR4FynMyD88RhoApaxillinchannel catfish virustriple-negative breast cancerInhibitorinhibitorinhibit

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