2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Melanocortin Receptor TRP Channel
  4. (±)-Eriodictyol

(±)-Eriodictyol  (Synonyms: (±)-Huazhongilexone; Dihydroluteolin)

Cat. No.: HY-N0637A Purity: 99.9%
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Handling Instructions Technical Support

(±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC50=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.

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

(±)-Eriodictyol

(±)-Eriodictyol Chemical Structure

CAS No. : 4049-38-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of (±)-Eriodictyol:

(±)-Eriodictyol Related Antibodies

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TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • Biological Activity

  • Purity & Documentation

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Description

(±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC50=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases[1][2][3][4][5].

IC50 & Target

rTRPV1

 

Cellular Effect
Cell Line Type Value Description References
B16-4A5 IC50
48 μM
Compound: 1
Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs by microplate reader analysis
Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs by microplate reader analysis
[PMID: 25987378]
Neutrophil IC50
1.4 μM
Compound: 5b
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of HOCl-induced oxidation of APF after 6 mins by fluorescence assay
[PMID: 23871908]
Neutrophil IC50
15.5 μM
Compound: 5b
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of superoxide anion radical-induced lucigenin oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
[PMID: 23871908]
Neutrophil IC50
18 μM
Compound: 5b
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of ROS-induced luminol oxidation incubated for 5 mins prior to PMA challenge by chemiluminescence assay
[PMID: 23871908]
Neutrophil IC50
4 μM
Compound: 5b
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
Inhibition of oxidative burst in PMA-stimulated human neutrophils assessed as inhibition of H2O2-induced oxidation of amplex red incubated for 5 mins prior to PMA challenge by fluorescence assay
[PMID: 23871908]
In Vitro

(±)-Eriodictyol inhibits LPS-induced inflammatory cytokine protein production and mRNA expression in C57BL/6 mouse bone marrow-derived macrophages[2].
(±)-Eriodictyol (3-300 nM) acts as a functional TRPV1 antagonist in rat spinal cord synaptosomes, inhibiting capsaicin-induced calcium influx with an IC50 of 44 nM, and does not alter baseline calcium levels on its own[3].
(±)-Eriodictyol (1-300 μM; 30 min) has cell-free antioxidant activity, scavenging ABTS radicals with an IC50 of 1.7 μM[3].
(±)-Eriodictyol (2.5-20 μM; 48 h) dose-dependently inhibits LPS-induced NO production in murine peritoneal macrophages, reducing NO to 31.8 μM at 20 μM over 48 h[4].
(±)-Eriodictyol (2.5-20 μM; 48 h) dose-dependently inhibits lysosomal enzyme activity in murine peritoneal macrophages, with significant suppression at 2.5, 5, 10, and 20 μM over 48 h[4].
(±)-Eriodictyol (6.25-50 μM; 1 h) exhibits dose-dependent cellular antioxidant activity in murine splenocytes and macrophages, with EC50 values of 13 μM and 14 μM, respectively, in the CAA assay[4].
(±)-Eriodictyol (5-20 μM; 24 h) dose-dependently suppresses the production of proinflammatory cytokines TNF-α and IL-8 in high glucose-stimulated rat RGC-5 retinal ganglial cells[5].
(±)-Eriodictyol (5-20 μM; 24 h) dose-dependently represses apoptosis in high glucose-stimulated rat RGC-5 retinal ganglial cells by modulating the expression of pro- and anti-apoptotic proteins[5].
(±)-Eriodictyol (5-20 μM; 24 h) enhances activation of the Nrf2/HO-1 pathway in high glucose-stimulated rat RGC-5 retinal ganglial cells, which is required for its protective effects against oxidative stress, inflammation, and apoptosis[5].

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

(±)-Eriodictyol Related Antibodies

Cell Viability Assay[5]

Cell Line: rat RGC-5 retinal ganglial cells
Concentration: 5-20 μM (pretreated, then incubated with HG); 5-20 μM (incubated with NG)
Incubation Time: 24 h
Result: Showed no effect on RGC-5 cell viability under NG conditions.
Improved RGC-5 cell viability in a dose-dependent manner under HG conditions, with significant increases observed at all tested concentrations.

ELISA Assay[5]

Cell Line: rat RGC-5 retinal ganglial cells
Concentration: 5-20 μM (pretreated, then incubated with HG)
Incubation Time: 24 h
Result: Dose-dependently reduced the HG-induced increases in TNF-α and IL-8 levels in RGC-5 cell supernatants.

Apoptosis Analysis[5]

Cell Line: rat RGC-5 retinal ganglial cells
Concentration: 5-20 μM (pretreated, then incubated with HG)
Incubation Time: 24 h
Result: Dose-dependently reduced HG-induced apoptosis.
Reversed the HG-induced changes in apoptosis-related protein expression: increased bcl-2 levels and decreased bax and cleaved caspase-3 levels.

Western Blot Analysis[5]

Cell Line: rat RGC-5 retinal ganglial cells
Concentration: 5-20 μM (pretreated, then incubated with HG); 20 μM (pretreated, then incubated with HG for Nrf2/HO-1 Western blot quantification)
Incubation Time: 24 h
Result: Enhanced HG-induced nuclear translocation of Nrf2 and HG-induced HO-1 protein expression in RGC-5 cells.
Knockdown of Nrf2 attenuated the protective effects of eriodictyol on HG-induced cell viability reduction, ROS production, TNF-α elevation, and apoptosis.
In Vivo

(±)-Eriodictyol (0.1-10 mg/kg; p.o.; daily; 10 days) dose-dependently reduces retinal inflammatory markers (TNF-α, eNOS) and plasma lipid peroxidation in streptozotocin-induced diabetic rats, with the 10 mg/kg dose suppressing blood-retinal barrier breakdown by 40% and lowering retinal VEGF and ICAM-1 levels[1].
(±)-Eriodictyol (30 mg/kg; p.o.; single dose; 2 days prior to LPS exposure) significantly attenuates LPS-induced acute lung injury in female C57BL/6 mice via anti-inflammatory and antioxidative mechanisms, including improved survival, reduced inflammatory cytokine production, and activation of the Nrf2-Trx1 pathway[2].
(±)-Eriodictyol (0.45-13.5 mg/kg; p.o.; single dose; 1 hour before capsaicin injection; 1-30 nmol/site; i.t.; single dose; 15 minutes before capsaicin injection) induces antinociception in intraplantar capsaicin-induced nociception in mice, with a maximal oral inhibition of 49% (ID50=2.3 mg/kg) and maximal intrathecal inhibition of 64% (ID50=2.2 nmol/site)[3].
(±)-Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before intrathecal capsaicin injection) inhibits intrathecal capsaicin-induced nociception in mice by 71%[3].
(±)-Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before nociception testing) fully reverses thermal hyperalgesia and reduces mechanical allodynia by 64% in CFA-induced inflammatory pain in mice[3].
(±)-Eriodictyol (4.5 mg/kg; p.o.; single dose; 1 hour before intraplantar capsaicin injection) prevents intraplantar capsaicin-induced spinal oxidative stress in mice by preserving non-protein thiol levels and blocking 3-nitrotyrosine formation[3].
(±)-Eriodictyol (combined with hesperidin and eriocitrin) enhances systemic antioxidant capacity and reduces markers of inflammation and oxidative stress in high-fat diet-fed C57BL/6J mice[5].

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

Animal Model: albino Swiss mice (three-month-old male, 25-35 g)[3]
Dosage: 4.5 mg/kg
Administration: p.o.; 1 hour before intrathecal capsaicin injection; single dose
Result: Produced a 71 ± 5% inhibition of intrathecal capsaicin-induced nociception.
Animal Model: albino Swiss mice (three-month-old male, 25-35 g)[3]
Dosage: 4.5 mg/kg
Administration: p.o.; 1 hour before nociception testing; single dose
Result: Fully reversed CFA-induced thermal hyperalgesia (100% inhibition).
Partially reduced CFA-induced mechanical allodynia (64 ± 7% inhibition).
Animal Model: albino Swiss mice (three-month-old male, 25-35 g)[3]
Dosage: 4.5 mg/kg
Administration: p.o.; 1 hour before intraplantar capsaicin injection; single dose
Result: Prevented the capsaicin-induced loss of non-protein thiols in the spinal cord.
Prevented the capsaicin-induced increase in spinal 3-NT levels.
Did not alter basal non-protein thiol or 3-NT levels in mice receiving intraplantar vehicle.
Animal Model: albino Swiss mice (three-month-old male, 25-35 g)[3]
Dosage: 4.5 mg/kg
Administration: p.o.; single dose
Result: Did not produce a significant change in rectal temperature at any measured time point compared to basal levels.
Molecular Weight

288.25

Formula

C15H12O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1CC(C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(O)=C13
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (346.92 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 3.4692 mL 17.3461 mL 34.6921 mL
5 mM 0.6938 mL 3.4692 mL 6.9384 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 and light). 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
=
Concentration
×
Volume
×
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 (8.67 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 (8.67 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).

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

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: 99.9%

SDS (396 KB)

COA (249 KB) HNMR (110 KB) CNMR (101 KB) RP-HPLC (106 KB) MS (130 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 (sealed storage, away from moisture and light). 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 3.4692 mL 17.3461 mL 34.6921 mL 86.7303 mL
5 mM 0.6938 mL 3.4692 mL 6.9384 mL 17.3461 mL
10 mM 0.3469 mL 1.7346 mL 3.4692 mL 8.6730 mL
15 mM 0.2313 mL 1.1564 mL 2.3128 mL 5.7820 mL
20 mM 0.1735 mL 0.8673 mL 1.7346 mL 4.3365 mL
25 mM 0.1388 mL 0.6938 mL 1.3877 mL 3.4692 mL
30 mM 0.1156 mL 0.5782 mL 1.1564 mL 2.8910 mL
40 mM 0.0867 mL 0.4337 mL 0.8673 mL 2.1683 mL
50 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7346 mL
60 mM 0.0578 mL 0.2891 mL 0.5782 mL 1.4455 mL
80 mM 0.0434 mL 0.2168 mL 0.4337 mL 1.0841 mL
100 mM 0.0347 mL 0.1735 mL 0.3469 mL 0.8673 mL
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(±)-Eriodictyol Related Classifications

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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.

Keywords:

(±)-Eriodictyol4049-38-1(±)-Huazhongilexone DihydroluteolinMelanocortin ReceptorTRP ChannelMC ReceptorTransient receptor potential channelsTRPV1B lymphocyteeNOSNrf2 pathwayVEGFICAM-1CTLrat RGC-5 retinal ganglial cellsNK cellTNF-αInhibitorinhibitorinhibit

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