1. Neuronal Signaling GPCR/G Protein Metabolic Enzyme/Protease Anti-infection Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
  3. Palmatine hydroxide

Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

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CAS No. : 131-04-4

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10 mM * 1 mL in DMSO
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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Palmatine hydroxide:

Top Publications Citing Use of Products

    Palmatine hydroxide purchased from MedChemExpress. Usage Cited in: Molecules. 2024 May 14;29(10):2304.

    The DPP-4 inhibitory activity of Palmatine chloride (10-7-10-3 M), demeasured using dose-response curves.

    Palmatine hydroxide purchased from MedChemExpress. Usage Cited in: Biol Res. 2020 Sep 14;53(1):39.  [Abstract]

    Palmatine chloride (PAL) (40 mg/kg; p.o.; once daily for 10 weeks) significantly decreased 2-h blood glucose level in HFD-fed SD rats.

    Palmatine hydroxide purchased from MedChemExpress. Usage Cited in: Biol Res. 2020 Sep 14;53(1):39.  [Abstract]

    Palmatine chloride (PAL) (40 mg/kg; p.o.; once daily for 10 weeks) significantly decreased blood insulin levels in HFD-fed SD rats.

    Palmatine hydroxide purchased from MedChemExpress. Usage Cited in: Biol Res. 2020 Sep 14;53(1):39.  [Abstract]

    Palmatine chloride (PAL) (40 mg/kg; p.o.; once daily for 10 weeks) restored the loss of β cell mass in HFD-fed SD rats, with predominantly increased area that stained positive for insulin.

    Palmatine hydroxide purchased from MedChemExpress. Usage Cited in: Biol Res. 2020 Sep 14;53(1):39.  [Abstract]

    Palmatine chloride (PAL) (40 mg/kg; p.o.; once daily for 10 weeks) remarkably reduced the apoptotic rates in HFD-fed SD rats.

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

    IC50 & Target

    IDO-1

    3 μM (IC50, HEK 293-hIDO-1)

    IDO-1

    157 μM (IC50, rhIDO-1)

    WNV NS2B-NS3

    96 μM (IC50)

    In Vitro

    Palmatine (0-100 μM; 42 h) suppresses WNV with an EC50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC50 values of 26.4 μM and 7.3 μM, respectively[3].
    Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation[5].
    Palmatine (0-704 μM; 24 h) reduces AURKA protein levels, induces G2/M phase arrest, and induces apoptosis in colon cancer cells via the mitochondrial associated pathway[5].

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

    Cell Proliferation Assay[5]

    Cell Line: HCT-116, SW480, HT-29
    Concentration: 0, 88, 176, 352, and 704 μM (HCT-116, SW480); 0, 141, 282, 564, and 1128 μM (HT-29)
    Incubation Time: 24, 48 and 72 h
    Result: Decreased cell viability in a dose-dependent manner.

    Western Blot Analysis[5]

    Cell Line: HCT-116, SW480, HT-29
    Concentration: 100 nM for HCT-116, 500 nM for SW480 and HT-29
    Incubation Time: 24, 48 and 72 h
    Result: Promoted the expression of apoptosis markers such as P53 / P73, Caspase3, and Caspase9. Reduced AURKA protein levels. Increased cyt. c in the cytoplasm while reduced Bcl2 and Bcl-xl in a dose-dependent manner.

    Cell Cycle Analysis[5]

    Cell Line: HCT-116, SW480
    Concentration: 88, 176, 352 and 704 μM
    Incubation Time: 24, 48 and 72 h
    Result: Induced G2/M phase arrest in a dose-dependent manner.

    Apoptosis Analysis[5]

    Cell Line: HCT-116, SW480
    Concentration: 88, 176, 352 and 704 μM
    Incubation Time: 24, 48 and 72 h
    Result: Induced apoptosis in a dose-dependent manner.
    In Vivo

    Palmatine (50 or 100 mg/kg; p.o.; daily for 7 days) ameliorates DSS (dextran sulfate sodium)-induced colitis and prevents infiltration of inflammatory cells[1].
    Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/Lipopolysaccharides (HY-D1056)-induced fulminant hepatic failure in mice[2].
    Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice[4].
    Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice[5].

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

    Animal Model: DSS- induced Colitis BALB/c mice model (8-week-old)[1]
    Dosage: 50 or 100 mg/kg
    Administration: Orally, daily, for 7 days
    Result: Ameliorated DSS-induced colitis and prevented infiltration of inflammatory cells; remarkably extended the colon length; significantly suppressed the colonic MPO activity. Decreased the levels of colonic inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); Protected mucosal integrity by modulating TJs protein and apoptosis proteins; Restored DSS-induced decreases of TJ protein ZO-1, ZO-2 and claudin-1; Reduced Bax expression and enhanced Bcl-2 expression at the dose of 100 mg/kg, prevented epithelial apoptosis and improved intestinal integrity. Prevented DSS-induced changes of gut microbiota in colitis mice.
    Animal Model: Male ICR mice (20–22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant hepatic failure model[2]
    Dosage: 25, 50, 100, or 200 mg/kg
    Administration: Intraperitoneal injection, 1 h before the GalN/LPS treatment
    Result: Attenuated the mortality and serum aminotransferase activities increased by GalN/LPS. Prevented the increase of serum TNF-α and augmented that of serum IL-10. Decreased the TNF-a mRNA expression and increased the IL-10 mRNA expression. Attenuated the apoptosis of hepatocytes.
    Animal Model: Swiss young male albino mice, with Scopolamine (HY-N0296)- and diazepam-induced amnesia model[4]
    Dosage: 0.1, 0.5, 1 mg/kg
    Administration: Intraperitoneal injection, 10 days
    Result: Significantly improved learning and memory of mice at 0.5 and 1 mg/kg and did not show any significant effect on locomotor activity of the mice. Significantly reversed scopolamine- and diazepam-induced amnesia in mice. Significantly reduced brain acetylcholinesterase activity of mice.
    Animal Model: BALB/c-nude mice, HCT-116 xenograft model[5]
    Dosage: 33.75, 67.5 and 135 mg/kg
    Administration: Oral administration, once a day for 26 days
    Result: The tumor volume and weight of the treatment group were significantly reduced.
    Molecular Weight

    369.41

    Formula

    C21H23NO5

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    COC(C=C1C2=CC3=CC=C4OC)=C(C=C1CC[N+]2=CC3=C4OC)OC.[OH-]

    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 : 15.62 mg/mL (42.28 mM; ultrasonic and warming and heat to 60°C; 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 2.7070 mL 13.5351 mL 27.0702 mL
    5 mM 0.5414 mL 2.7070 mL 5.4140 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.

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

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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.64%

    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 2.7070 mL 13.5351 mL 27.0702 mL 67.6755 mL
    5 mM 0.5414 mL 2.7070 mL 5.4140 mL 13.5351 mL
    10 mM 0.2707 mL 1.3535 mL 2.7070 mL 6.7675 mL
    15 mM 0.1805 mL 0.9023 mL 1.8047 mL 4.5117 mL
    20 mM 0.1354 mL 0.6768 mL 1.3535 mL 3.3838 mL
    25 mM 0.1083 mL 0.5414 mL 1.0828 mL 2.7070 mL
    30 mM 0.0902 mL 0.4512 mL 0.9023 mL 2.2558 mL
    40 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6919 mL
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    Product Name:
    Palmatine hydroxide
    Cat. No.:
    HY-N0110B
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