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    CAS No. 2543-94-4 Price $388 / 10mg
    Catalog No.CFN90495Purity>=98%
    Molecular Weight300.3Type of CompoundCoumarins
    FormulaC17H16O5Physical DescriptionPowder
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    Description: Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro; it shows cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
    Targets: NO | Akt | PKC | TNF-α | GABA Receptor | ERK
    In vitro:
    Int Immunopharmacol. 2008 May;8(5):670-8.
    Hesperidin, hesperidin methyl chalone and phellopterin from Poncirus trifoliata (Rutaceae) differentially regulate the expression of adhesion molecules in tumor necrosis factor-alpha-stimulated human umbilical vein endothelial cells.[Pubmed: 18387509 ]
    The fruits of Poncirus trifoliata (L.) are widely used in Oriental medicine to treat allergic inflammation. Recently, several active compounds including hesperidin, hesperidin methyl chalone and Phellopterin from P. trifoliata (Rutaceae) were isolated and characterized.
    The goal of this study was to investigate the differential effect of hesperidin, hesperidin methyl chalone and Phellopterin derived from P. trifoliata (Rutaceae) on the induction of intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1) by TNF-alpha and the possible molecular mechanisms by which they differentially regulate ICAM-1 and VCAM-1 expressions. Stimulation of human umbilical vein endothelial cells (HUVECs) with TNF-alpha resulted in the increase of ICAM-1 and VCAM-1 expressions, while pretreatment with the three components completely inhibited VCAM-1 expression in a dose-dependent manner but had no effect on ICAM-1 expression. All three compounds failed to block TNF-alpha-induced phosphorylation of ERK1/2, which is involved in regulating ICAM-1 production by TNF-alpha. Furthermore, they efficiently inhibited the phosphorylation of Akt and PKC, suggesting that Akt or PKC pathways are an important target by which these compounds regulate TNF-alpha-induced VCAM-1 but not ICAM-1. Additionally, treatment with these chemicals also inhibited U937 monocyte adhesion to HUVECs stimulated with TNF-alpha. Interestingly, the inhibitory effect of hesperidin, hesperidin methyl chalone and Phellopterin on monocyte adhesion to HUVECs was recapitulated by transfecting cells with VCAM-1 siRNA.
    Taken together, hesperidin, hesperidin methyl chalone and Phellopterin reduce TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
    Neurosci Lett. 1996 Nov 29;219(3):151-4.
    Characterisation of the furanocoumarin phellopterin as a rat brain benzodiazepine receptor partial agonist in vitro.[Pubmed: 8971802]

    Phellopterin, a naturally occurring furanocoumarin found in the roots of Angelica dahurica, inhibits [3H]diazepam and ethyl 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4] benzodiazepine-3-carboxylate ([3H]Ro 15-1788) binding to the benzodiazepine site of the rat brain gamma-aminobutyric acidA (GABAA) receptor in vitro with IC50 values of 400 and 680 nM, respectively. Two other naturally occurring furanocoumarins, byakangelicol and imperatorin were significantly less potent, with IC50 values for inhibition of [3H]diazepam binding of 8.0 and 12.3 microM, respectively. Scatchard plot analysis showed that the inhibitory activity of Phellopterin was due to competitive inhibition of the benzodiazepine ligand binding.
    The results of GABA- and t-butylbicyclophosphorothionate (TBPS)-shift assays suggest that Phellopterin is a partial agonist of the central benzodiazepine receptors in vitro.
    Phellopterin Description
    Source: The roots of Saposhnikovia divaricata
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.33 mL 16.65 mL 33.3 mL 66.6001 mL 83.2501 mL
    5 mM 0.666 mL 3.33 mL 6.66 mL 13.32 mL 16.65 mL
    10 mM 0.333 mL 1.665 mL 3.33 mL 6.66 mL 8.325 mL
    50 mM 0.0666 mL 0.333 mL 0.666 mL 1.332 mL 1.665 mL
    100 mM 0.0333 mL 0.1665 mL 0.333 mL 0.666 mL 0.8325 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Cell Research:
    J Asian Nat Prod Res. 2012;14(10):956-65.
    Biotransformation products of phellopterin by rat liver microsomes and the inhibition on NO production in LPS-activated RAW264.7 cells.[Pubmed: 23046467]

    Four new coumarins (2',3'-dihydroxyPhellopterin, E-5-methoxytrichoclin acetate, Z-5-methoxytrichoclin acetate, and E-5-methoxytrichoclin) and three known coumarins (byakangelicol, byakangelicin, and Z-5-methoxytrichoclin) were produced by liver microsomes from rats pre-treated with sodium phenobarbital. The chemical structures were elucidated on the basis of their spectroscopic data. The inhibitory activities of nitric oxide (NO) production in lipopolysaccharide-activated macrophage-like cell line RAW264.7 were tested.
    The main biotransformation product, byakangelicin, showed inhibitory activities of NO production with the IC₅₀ value of 217.83 μM, whereas the parent compound Phellopterin showed cytotoxic effect on RAW264.7 cell at the concentration from 40 to 400 μM.