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

Palmatine 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities.

It is advisable to consider the salt form (Palmatine chloride) that retains the same biological activity.

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

CAS No. : 3486-67-7

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Top Publications Citing Use of Products

    Palmatine 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 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 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 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 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

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    Description

    Palmatine 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 can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

    IC50 & Target[1]

    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 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 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 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

    352.40

    Formula

    C21H22NO4+

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    COC1=C(OC)C2=C[N+]3=C(C4=CC(OC)=C(OC)C=C4CC3)C=C2C=C1

    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)

    Purity & Documentation
    References
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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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