1. MAPK/ERK Pathway
  2. p38 MAPK
  3. Rhamnocitrin

Rhamnocitrin is an anti-inflammatory and antioxidant agent that targets STIM-1, NFATc3 and MAPK pathways and can scavenge DPPH (IC50=28.38 mM). Rhamnocitrin selectively inhibits oxidative stress and inflammatory responses in vascular endothelial cells and neurons. Rhamnocitrin up-regulates miR-185 to inhibit STIM-1-mediated store-operated calcium entry (SOCE), thereby blocking NFATc3 nuclear translocation and downstream inflammatory factor expression, while inducing heme oxygenase HO-1 expression and regulating the ERK/p38 MAPK pathway, inhibiting antioxidant and pro-inflammatory cytokines (such as IL-6, IL-8) and adhesion molecules (such as ICAM-1, VCAM-1). Rhamnocitrin can be used in the study of endothelial-related inflammatory diseases (such as sepsis, acute lung injury, atherosclerosis) and neuroprotection (such as oxidative damage of PC12 cells).

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

CAS No. : 569-92-6

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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
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Rhamnocitrin:

Top Publications Citing Use of Products
Cell Proliferation/Viability Assay
IF
Flow Cytometry
WB

    Rhamnocitrin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Nov 16;14(1):28287.  [Abstract]

    MDCK and A549 cells were incubated with different concentrations of Rhamnocitrin (RH) (0-100 µM). MDCK and A549 cell viability after 48 and 24 h of treatment, respectively, were measured via CCK-8 assay.

    Rhamnocitrin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Nov 16;14(1):28287.  [Abstract]

    Effects of Rhamnocitrin (RH) (25, 50, 100 μM) on the apoptosis of H3N2-infected MDCK cells.

    Rhamnocitrin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Nov 16;14(1):28287.  [Abstract]

    The effect of Rhamnocitrin (RH) (25, 50, 100 μM) on apoptotic A549 cells infected with H3N2 virus for 24 h was detected by flow cytometry analysis

    Rhamnocitrin purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Nov 16;14(1):28287.  [Abstract]

    Protein expressions of TBK1, phosphp-TBK1 were detected via western blot analysis treated with Rhamnocitrin (RH) (25, 50, 100 μM).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rhamnocitrin is an anti-inflammatory and antioxidant agent that targets STIM-1, NFATc3 and MAPK pathways and can scavenge DPPH (IC50=28.38 mM). Rhamnocitrin selectively inhibits oxidative stress and inflammatory responses in vascular endothelial cells and neurons. Rhamnocitrin up-regulates miR-185 to inhibit STIM-1-mediated store-operated calcium entry (SOCE), thereby blocking NFATc3 nuclear translocation and downstream inflammatory factor expression, while inducing heme oxygenase HO-1 expression and regulating the ERK/p38 MAPK pathway, inhibiting antioxidant and pro-inflammatory cytokines (such as IL-6, IL-8) and adhesion molecules (such as ICAM-1, VCAM-1). Rhamnocitrin can be used in the study of endothelial-related inflammatory diseases (such as sepsis, acute lung injury, atherosclerosis) and neuroprotection (such as oxidative damage of PC12 cells)[1][2][3][4].

    In Vitro

    Rhamnocitrin (40-80 μM; 48 h) significantly reduces apoptosis in serum deprivation-induced rat adrenal pheochromocytoma PC12 cells, and has no significant effect on STIM-1/Orai-1-mediated SOCE and downstream NFATc3 signaling[2].
    Rhamnocitrin (0.1-10 μM; 24 h) inhibits the expression of IL-6, IL-8, MCP-1, ICAM-1, VCAM-1 and PAI-1 in a concentration-dependent manner in LPS-induced human umbilical vein endothelial cells (HUVECs) experiments, and inhibits STIM-1-mediated store-operated calcium entry (SOCE)[3].

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

    Western Blot Analysis[3]

    Cell Line: Human umbilical vein endothelial cells (HUVECs)
    Concentration: 0.1 μM, 1 μM, 10 μM
    Incubation Time: 24 h pretreatment + 6 h LPS stimulation
    Result: Dose-dependently reduced protein levels of ICAM-1, VCAM-1, and PAI-1 induced by LPS.
    Significantly suppressed mRNA expressions of IL-6, IL-8, and MCP-1 at 1 μM and 10 μM.
    Attenuated nuclear translocation of NFATc3, a downstream target of SOCE in a concentration-dependent manner.
    Cell Viability**: No significant cytotoxicity was observed at concentrations ≤10 μM (CCK-8 assay).

    Cell Viability Assay[2]

    Cell Line: Rat pheochromocytoma PC12 cells
    Concentration: 40 μM, 60 μM, 80 μM
    Incubation Time: 48 h
    Result: Cell Viability: Dose-dependent increased in cell viability, with 60 μM and 80 μM groups significantly higher than the vehicle control.
    Cell Apoptosis: Resulted a reduction in sub-G0/G1 phase cells (apoptotic cells) at 60 μM and 80 μM, indicating decreased apoptosis.
    WB: Persistently attenuated of p38 MAPK, while increased ERK1/2 activation transiently at 60 μM.
    In Vivo

    After oral administration of 10 mL/kg A. complanatus extract (equivalent to 17.6 mg/kg Rhamnocitrin) to rats, collects blood (approximately 0.3 mL) at 0, 0.083, 0.167, 0.25, 0.333, 0.5, 0.75, 1, 2, 4, 6, 9, and 12 hours after administration from the ocular vein for analysis, under ether anesthesia. The results shows that the plasma concentration of Rhamnocitrin reached its maximum at 0.65 hours, with an average Cmax of 29.57 ng/mL[1].

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

    Molecular Weight

    300.26

    Formula

    C16H12O6

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1C(O)=C(C2=CC=C(O)C=C2)OC3=CC(OC)=CC(O)=C13

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (333.04 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 3.3304 mL 16.6522 mL 33.3045 mL
    5 mM 0.6661 mL 3.3304 mL 6.6609 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 (protect from light). 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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    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: ≥ 2.08 mg/mL (6.93 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 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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    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 (protect from 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: 99.67%

    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 (protect from 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 3.3304 mL 16.6522 mL 33.3045 mL 83.2612 mL
    5 mM 0.6661 mL 3.3304 mL 6.6609 mL 16.6522 mL
    10 mM 0.3330 mL 1.6652 mL 3.3304 mL 8.3261 mL
    15 mM 0.2220 mL 1.1101 mL 2.2203 mL 5.5507 mL
    20 mM 0.1665 mL 0.8326 mL 1.6652 mL 4.1631 mL
    25 mM 0.1332 mL 0.6661 mL 1.3322 mL 3.3304 mL
    30 mM 0.1110 mL 0.5551 mL 1.1101 mL 2.7754 mL
    40 mM 0.0833 mL 0.4163 mL 0.8326 mL 2.0815 mL
    50 mM 0.0666 mL 0.3330 mL 0.6661 mL 1.6652 mL
    60 mM 0.0555 mL 0.2775 mL 0.5551 mL 1.3877 mL
    80 mM 0.0416 mL 0.2082 mL 0.4163 mL 1.0408 mL
    100 mM 0.0333 mL 0.1665 mL 0.3330 mL 0.8326 mL
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      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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