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  3. Ellagic acid

Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.

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

CAS No. : 476-66-4

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Based on 22 publication(s) in Google Scholar

Other Forms of Ellagic acid:

Top Publications Citing Use of Products

    Ellagic acid purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2025 May 19:e70064.  [Abstract]

    Representative fluorescent images showing the internalisation of Dil‐labelled EVs and EA‐sEVs by HG‐HDFs and HG‐HEKs at 6 h; scale bar, 50 μm. Blue: DAPI, red: Dil, green: Phalloidine.

    Ellagic acid purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Jun;13(6):2680-2700.

    After treatment with different concentrations of Ellagic acid (0-20 μM) for 24 h, the expression of SIRT6, SGK1, H3K9 and H3K56 in primary cardiomyocytes isolated from WT mice and LLC cells was examined by Western blotting. β-Actin was used as a loading control. Semiquantitative analyses of bands were performed using ImageJ software.

    Ellagic acid purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Jun;13(6):2680-2700.

    Primary cardiomyocytes isolated from WT mice and LLC cells were transfected with SIRT6 siRNA or control siRNA. After pre-treated with Ellagic acid (10 μmol/L) for 24 h, Dox (0.5 μmol/L) was added to culture medium for subsequent 24 h, and apoptosis was analyzed by TUNEL assays. Representative images are shown (scale bar = 100 μm). The TUNEL-positive rates were quantified blindly in 5 images from different fields.

    Ellagic acid purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Jun;13(6):2680-2700.

    Wild-type C57BL/6 mice were inoculated subcutaneously with 1.5 × 106 LLC-Luc cells (LLC cells stably expressing the luciferase gene). After tumors became visible (approximately 7 days), the tumor-bearing mice were treated with Dox (10 mg/kg/week, i.v.) or/and Ellagic acid (100 mg/kg/2 days, i.g.) for 2 weeks. Tumor volume was visualized using the IVIS Imaging System before and after treatment, and representative bioluminescence images and quantitative analyses of the tumor-bearing mice are shown.

    Ellagic acid purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Jun;13(6):2680-2700.

    Wild-type C57BL/6 mice were inoculated subcutaneously with 1.5 × 106 LLC-Luc cells (LLC cells stably expressing the luciferase gene). After tumors became visible (approximately 7 days), the tumor-bearing mice were treated with Dox (10 mg/kg/week, i.v.) or/and Ellagic acid (100 mg/kg/2 days, i.g.) for 2 weeks. Cell morphology, fibrosis and apoptosis in the cardiac tissue of the tumor-bearing mice were examined by H&E, Masson and TUNEL staining, respectively. Cell morphology, proliferation and apoptosis and in the tumors were measured by H&E, Ki67 immunofluorescence and TUNEL staining, respectively.

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    Description

    Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.

    IC50 & Target[1]

    CK2

    40 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    Erythrocyte IC50
    0.32 mM
    Compound: 6
    Anticomplement activity in rabbit erythrocytes assessed as concentration required for 50% hemolytic inhibition by alternative pathway pretreated for 10 mins with normal human serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
    Anticomplement activity in rabbit erythrocytes assessed as concentration required for 50% hemolytic inhibition by alternative pathway pretreated for 10 mins with normal human serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
    [PMID: 29631958]
    Erythrocyte IC50
    0.32 mM
    Compound: 6
    Anticomplement activity in sheep erythrocytes assessed as concentration required for 50% hemolytic inhibition by classic pathway pretreated for 10 mins with guinea pig serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
    Anticomplement activity in sheep erythrocytes assessed as concentration required for 50% hemolytic inhibition by classic pathway pretreated for 10 mins with guinea pig serum followed by erythrocyte addition measured after 30 mins by spectrophotometeric method
    [PMID: 29631958]
    HEK293 IC50
    2.93 μM
    Compound: EA
    Inhibition of catalytic activity of human recombinant FLAG-tagged ppGalNAcT2 W282A mutant expressed in HEK293 cells using EA2 peptide as substrate by HPLC-based enzyme assay
    Inhibition of catalytic activity of human recombinant FLAG-tagged ppGalNAcT2 W282A mutant expressed in HEK293 cells using EA2 peptide as substrate by HPLC-based enzyme assay
    [PMID: 31227364]
    HT-29 EC50
    0.11 μM
    Compound: Ellagic acid
    Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
    Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
    [PMID: 24900447]
    HT-29 IC50
    0.1 μM
    Compound: Ellagic acid
    Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
    Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
    [PMID: 24900447]
    HUVEC IC50
    > 165 μM
    Compound: 9
    Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by fluorescence based assay
    Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 48 hrs by fluorescence based assay
    [PMID: 37122550]
    MDA-MB-231 IC50
    27.38 μM
    Compound: 4
    Cytotoxicity against human MDA-MB-231 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
    Cytotoxicity against human MDA-MB-231 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
    [PMID: 33359608]
    MIA PaCa-2 IC50
    149.83 μM
    Compound: 4
    Cytotoxicity against human MIA PaCa-2 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
    Cytotoxicity against human MIA PaCa-2 cells expressing CD73 assessed as reduction in cell viability by CCK8 assay
    [PMID: 33359608]
    Oocyte IC50
    270 nM
    Compound: ellagic acid
    TP_TRANSPORTER: inhibition of ochratoxin A uptake (ochratoxin A / 1uM) in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of ochratoxin A uptake (ochratoxin A / 1uM) in Xenopus laevis oocytes
    [PMID: 15870380]
    Panel NCI-60 (60 carcinoma cell lines) GI50
    10 nM
    Compound: Ellagic acid
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program
    [PMID: 15743190]
    RAW264.7 IC50
    35.7 μM
    Compound: 24
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis
    [PMID: 24679441]
    RAW264.7 IC50
    > 50 μM
    Compound: 12
    Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by by Griess assay
    Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 2 hrs followed by LPS stimulation and measured after 24 hrs by by Griess assay
    [PMID: 31419126]
    RAW264.7 IC50
    > 50 μM
    Compound: 24
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA
    [PMID: 24679441]
    SH-SY5Y IC50
    300 μM
    Compound: EA
    Inhibition of beta amyloid in human SH-SY5Y cells
    Inhibition of beta amyloid in human SH-SY5Y cells
    [PMID: 31563012]
    Sf9 IC50
    0.25 μM
    Compound: EA
    Inhibition of human recombinant IGF1R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant IGF1R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.26 μM
    Compound: EA
    Inhibition of human recombinant TIE2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant TIE2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.34 μM
    Compound: EA
    Inhibition of human recombinant INS-R expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant INS-R expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.51 μM
    Compound: EA
    Inhibition of human recombinant ARK5 expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
    Inhibition of human recombinant ARK5 expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.58 μM
    Compound: EA
    Inhibition of human recombinant MET expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant MET expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.69 μM
    Compound: EA
    Inhibition of human recombinant EGF-R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant EGF-R expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.79 μM
    Compound: EA
    Inhibition of human recombinant VEGF-R2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant VEGF-R2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    0.8 μM
    Compound: EA
    Inhibition of human recombinant SRC expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant SRC expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    1.09 μM
    Compound: EA
    Inhibition of human recombinant CDK4/CyclinD1 expressed in Sf9 cells using RB-CTF as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant CDK4/CyclinD1 expressed in Sf9 cells using RB-CTF as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    1.3 μM
    Compound: EA
    Inhibition of human recombinant PDGFRbeta expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant PDGFRbeta expressed in Sf9 cells using poly(A,E,K,Y)6:2:5:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    1.54 μM
    Compound: EA
    Inhibition of human recombinant VEGF-R3 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant VEGF-R3 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    1.76 μM
    Compound: EA
    Inhibition of human recombinant B-RAF expressed in Sf9 cells using MEK1 KM as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant B-RAF expressed in Sf9 cells using MEK1 KM as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    1.83 μM
    Compound: EA
    Inhibition of human recombinant EPHB4 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant EPHB4 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    2.37 μM
    Compound: EA
    Inhibition of human recombinant COT expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
    Inhibition of human recombinant COT expressed in Sf9 cells assessed as autophosphorylation after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    2.48 μM
    Compound: EA
    Inhibition of human recombinant aurora-A expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant aurora-A expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    2.5 μM
    Compound: EA
    Inhibition of human recombinant aurora-B expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant aurora-B expressed in Sf9 cells using tetra(LRRWSLG) as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    2.97 μM
    Compound: EA
    Inhibition of human recombinant SAK expressed in Sf9 cells using p38alpha-KRKR as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant SAK expressed in Sf9 cells using p38alpha-KRKR as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    3.11 μM
    Compound: EA
    Inhibition of human recombinant FAK expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant FAK expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    3.34 μM
    Compound: EA
    Inhibition of human recombinant AKT1 expressed in Sf9 cells using GSK3(14-27) as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant AKT1 expressed in Sf9 cells using GSK3(14-27) as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    3.34 μM
    Compound: EA
    Inhibition of human recombinant PLK1 expressed in Sf9 cells using casein as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant PLK1 expressed in Sf9 cells using casein as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    3.39 μM
    Compound: EA
    Inhibition of human recombinant CDK2/CyclinA expressed in Sf9 cells using histone H1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant CDK2/CyclinA expressed in Sf9 cells using histone H1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    Sf9 IC50
    3.54 μM
    Compound: EA
    Inhibition of human recombinant ERBB2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    Inhibition of human recombinant ERBB2 expressed in Sf9 cells using poly(E,Y)4:1 as substrate after 80 mins by scintillation counting
    [PMID: 22377675]
    U2OS EC50
    2.96 μM
    Compound: Ellagic acid
    Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
    Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
    [PMID: 24900447]
    In Vitro

    Ellagic acid is a potent CK2 inhibitor, with an IC50 of 40 nM and a Ki of 20 nM. Ellagic acid also blocks other kinases such as LYN, PKA, SYK, GSK3, FGR and CK1, with IC50s of 2.9, 3.5, 4.3, 7.5, 9.4 and 13.0 μM, respectively, and shows no obvious effects on DYRK1a, CSK, NPM-ALK, RET and FLT3 (IC50s > 40 μM). Ellagic acid (5-100 μM) shows inhibitory activities against Karpas299, SUDHL1, SR786, and FE-PD cell lines[1]. Ellagic acid (10 μM) exhibits cytotoxic effects on MCF-7 cells after treatment of radiation. Ellagic acid (10 μM) in combination with Irradiation (IR) significantly abridges the capacity of MCF-7 cells to form colonies equated with individual treatments. Ellagic acid with IR also induces cell apoptosis, and facilitates the upregulation of pro-apopttotic Bax and downregulation of Bcl-2 in MCF-7 cells[3].

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

    In Vivo

    Ellagic acid (EA; 10 mg/kg/day; p.o., 14 days) strongly decreases MDA brain content by 17%, and reduces the levels of brain TNF-α by 42% in rats. Ellagic acid markedly increases the reduced brain contents of 5-HT (39%), dopamine (DA, 71%), and norepinephrine (NE, 77%). Ellagic acid (10 mg/kg, p.o., 14 days) causes decreased histopathological changes induced by Doxorubicin in rats[2].

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

    Molecular Weight

    302.19

    Formula

    C14H6O8

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C1C2=CC(O)=C(O)C(O3)=C2C4=C(C3=O)C=C(O)C(O)=C4O1

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 2 mg/mL (6.62 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 3.3092 mL 16.5459 mL 33.0918 mL
    5 mM 0.6618 mL 3.3092 mL 6.6184 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.75%

    References
    Kinase Assay
    [1]

    CK2 and CK1 phosphorylation assays are carried out at 37°C in the presence of increasing amounts of each inhibitor (Ellagic acid) in a final volume of 25 µL containing 50 mM, Tris-HCl pH 7.5, 100 mM NaCl, 12 mM MgCl2, 0.02 mM [33P-ATP] (500-1000 cpm/pmol), unless otherwise indicated. The phosphorylatable substrates are the synthetic peptide substrate RRRADDSDDDDD (100 µM) and RRKHAAIGDDDDAYSITA (200 µM) for CK2 and CK1, respectively. Reaction started with the addition of the kinase and is stopped after 10 min. by addition of 5 µL of 0.5 M orthophosphoric acid before spotting aliquots onto phosphocellulose filters. Filters are washed in 75 mM phosphoric acid substrate following SDS-PAGE of the radiolabeled samples. DYRK1A, assayed on the peptide RRRFRPASPLRGPPK, and tyrosine kinase activities are determined[1].

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

    Cell Assay
    [1]

    ALCL cell viability is measured by MTT assay. Briefly, 0.1 × 105 cells are seeded onto 96-well microculture plates 12 hrs before adding ellagic acid. The cells are grown in 200 µL of complete RPMI-1640 medium, under standard tissue-culture conditions, in the presence or absence of the drug (Ellagic acid) for 48 hours. Twenty µL of MTT solution (5 mg/mL) are then added to the cell suspension for 4h. The intracellular formazan crystals are dissolved with 150 µL of DMSO and optical density, measured on a spectrophotometer at 540 nm, represents the mean (± SD) of triplicate cultures[1].

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

    Animal Administration
    [2]

    Fifty male adult Sprague-Dawley rats are divided randomly into five groups as follow: Group (1) receives corn oil orally as a vehicle and served as normal control. Group (2) receives doxorubicin (DOX) injection (5 mg/kg, i.p.) twice a week for 14 days. Group (3) receives Ellagic acid (10 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.) twice a week for 14 days. Group (4) receives rosmarinic acid (RA; 75 mg/kg, p.o.; daily) for 14 days and DOX (5 mg/kg, i.p.) twice a week for 14 days. Group (5) receives Ellagic acid (10 mg/kg, p.o.; daily) with RA (75 mg/kg, p.o.; daily) for 14 days and DOX injection (5 mg/kg, i.p.) twice a week for 14 days[2].

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

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3092 mL 16.5459 mL 33.0918 mL 82.7294 mL
    5 mM 0.6618 mL 3.3092 mL 6.6184 mL 16.5459 mL
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    Product Name:
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    Cat. No.:
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