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    Chrysosplenetin
    Chrysosplenetin
    Information
    CAS No. 603-56-5 Price $268 / 20mg
    Catalog No.CFN97026Purity>=98%
    Molecular Weight374.4 Type of CompoundFlavonoids
    FormulaC19H18O8Physical DescriptionYellow powder
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    According to end customer requirements, ChemFaces provide solvent format. This solvent format of product intended use: Signaling Inhibitors, Biological activities or Pharmacological activities.
    Size /Price /Stock 10 mM * 1 mL in DMSO / $96.2 / In-stock
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    Chrysosplenetin

    Chrysosplenetin
    Product Name Chrysosplenetin
    CAS No.: 603-56-5
    Catalog No.: CFN97026
    Molecular Formula: C19H18O8
    Molecular Weight: 374.4 g/mol
    Purity: >=98%
    Type of Compound: Flavonoids
    Physical Desc.: Yellow powder
    Targets: P450 (e.g. CYP17) | Antifection
    Source: The herbs of Laggera pterodonta
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Price: $268 / 20mg
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  • Related Screening Libraries
    Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
    10 mM * 1 mL in DMSO / Inquiry / In-stock
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  • Biological Activity
    Description: Chrysosplenetin is a metabolic inhibitor of artemisinin, it has strong activity in vitro against EV71 with low cytotoxicity. Co-administration of artemisinin(ART) with chrysosplenetin(CHR) in ratio of 1:2 achieved a synergic anti-malarial effect partly because of the noncompetitive or uncompetitive inhibition of CHR of drug-metabolism enzymes, especially CYP3A which is closely related to the auto-induction of ART.
    Targets: P450 (e.g. CYP17) | Antifection
    In vitro:
    Zhongguo Zhong Yao Za Zhi. 2013 Oct;38(19):3363-7.
    Determination of chrysosplenetin, metabolic inhibitor of artemisinin, in rat plasma by UPLC-ms/MS and study on its pharmacokinetics.[Pubmed: 24422409]

    METHODS AND RESULTS:
    The study aimed to develop the assay of Chrysosplenetin (CHR), a metabolic inhibitor of artemisinin by UPLC-MS/MS in rat plasma and investigate the pharmacokinetics parameters of Chrysosplenetin.The assay was linear in the range 5-5 000 microg L-1 (r =0. 999 3) with recoveries in the range from 69. 0% to 81.2% and satisfied inter-, intra- precision and accuracy. Chrysosplenetin after oral administration is not easy to absorb with double or multimodal peak phenomenon. The t1/2 of Chrysosplenetin after intravenous injection was very short and that of low, medium, and high dosage was (17. 01 +/- 8. 06) , (24. 62 +/- 4. 59), (28. 46+/- 4. 63) min, respectively.
    CONCLUSIONS:
    The developed method was special, rapid, and sensitive for determination of Chrysosplenetin pharmacokinetics.
    Eur J Pharm Sci. 2011 Oct 9;44(3):392-8.
    Inhibition of enterovirus 71 replication by chrysosplenetin and penduletin.[Pubmed: 21914477]
    In recent years, enterovirus 71 (EV71) infections have caused an increasing epidemic in young children, accompanying with more severe nervous system disease and more deaths. Unfortunately, there is no specific medication for it so far.
    METHODS AND RESULTS:
    Here we investigated the anti-EV71 activity of Chrysosplenetin and penduletin, two o-methylated flavonols isolated from the leaves of Laggera pterodonta. These two compounds were found to have strong activity in vitro against EV71 with low cytotoxicity. In the cytopathic effect (CPE) inhibition assays, both plaque reduction assay and virus yield inhibition assay, the compounds showed a similar 50% inhibitory concentration (IC(50)) value of about 0.20 μM.
    CONCLUSIONS:
    The selectivity indices (SI) of Chrysosplenetin and penduletin were 107.5 and 655.6 in African green monkey kidney (Vero) cells, and 69.5 and 200.5 in human rhabdomyosarcoma (RD) cells, accordingly.
    In vivo:
    Malaria J., 2015, 14(1):1-13.
    Impact of chrysosplenetin on the pharmacokinetics and anti-malarial efficacy of artemisinin against Plasmodium berghei as well as in vitro CYP450 enzymatic activities in rat liver microsome.[Pubmed: 26537009]
    Artemisinin (ART) is an efficacious and safe anti-malarial drugs but has low oral bioavailability and auto-induction profiles during multiple dosing. The pharmacokinetic disadvantages have been found to partially depend on the induction of cytochrome P-450 enzymes by ART and resulted in the therapeutic failure due to insufficient drug levels.
    METHODS AND RESULTS:
    The present study, therefore, investigated the impacts of Chrysosplenetin (CHR), a polymethoxylated flavonoid from Artemisia annua, on the pharmacokinetics and the anti-malarial efficacy of ART against Plasmodium berghei. The inhibition of CHR on enzymatic activity of CYP1A2, CYP2A, CYP2C19, CYP2D6, CYP2E1, and CYP3A in rat liver microsome was also investigated. IC50, Km, Ki, and inhibitory type of CHR were respectively calculated. Co-administration of ART with CHR in ratio of 1:2 achieved a synergic anti-malarial effect partly because of the noncompetitive or uncompetitive inhibition of CHR of drug-metabolism enzymes, especially CYP3A which is closely related to the auto-induction of ART.
    Chrysosplenetin Description
    Source: The herbs of Laggera pterodonta
    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 2.6709 mL 13.3547 mL 26.7094 mL 53.4188 mL 66.7735 mL
    5 mM 0.5342 mL 2.6709 mL 5.3419 mL 10.6838 mL 13.3547 mL
    10 mM 0.2671 mL 1.3355 mL 2.6709 mL 5.3419 mL 6.6774 mL
    50 mM 0.0534 mL 0.2671 mL 0.5342 mL 1.0684 mL 1.3355 mL
    100 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.5342 mL 0.6677 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.
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