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  • 荜茇酰胺

    Piplartine

    荜茇酰胺
    产品编号 CFN96137
    CAS编号 20069-09-4
    分子式 = 分子量 C17H19NO5 = 317.3
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The herbs of Piper longum L.
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
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    产品名称 产品编号 CAS编号 包装 QQ客服
    荜茇酰胺 CFN96137 20069-09-4 10mg QQ客服:1413575084
    荜茇酰胺 CFN96137 20069-09-4 20mg QQ客服:1413575084
    荜茇酰胺 CFN96137 20069-09-4 50mg QQ客服:1413575084
    荜茇酰胺 CFN96137 20069-09-4 100mg QQ客服:1413575084
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • Hamdard University (India)
  • Celltrion Chemical Research Institute (Korea)
  • University of Limpopo (South Africa)
  • Universidad Veracuzana (Mexico)
  • Universiti Putra Malaysia(UPM) (Malaysia)
  • Kamphaengphet Rajabhat University (Thailand)
  • Center for protein Engineering (CIP) (Belgium)
  • The University of Newcastle (Australia)
  • Tokyo Woman's Christian University (Japan)
  • University of the Basque Country (Spain)
  • Anna University (India)
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  • Massachusetts General Hospital (USA)
  • Lodz University of Technology (Poland)
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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Food Chemistry: X.2022, 2022.100270
  • J Biomol Struct Dyn.2023, 1-21.
  • J AOAC Int.2021, 104(6):1634-1651.
  • J Chromatogr Sci.2020, 58(6):485-493.
  • Institute of Food Science & Technology2021, 56(11).
  • Molecules.2020, 25(20):4851.
  • Life (Basel).2021, 11(12):1399.
  • Process Biochemistry2019, 85:106-115
  • Anat Rec (Hoboken).2021, 304(2):323-332.
  • Theoretical and Experimental Plant Physiology 2022, 34,53-62
  • Biochem Pharmacol.2020, 178:114083
  • Nat Prod Commun.2014, 9(5):679-82
  • Food Chem.2020, 332:127412
  • J of the Korean Society of Cosmetics and Cosmetology2018, 399-406
  • Plant Physiol Biochem.2023, 201:107795.
  • Korean J Environ Agric.2018, 37(4):260-267
  • Arch Biochem Biophys.2018, 644:93-99
  • The Journal of Supercritical Fluids2021, 176:105305.
  • Plant Pathology2022, 13527
  • Biomolecules.2021, 11(10):1537.
  • J Biochem Mol Toxicol.2020, 34(7):e22489.
  • Analytical methods2019, 11(6)
  • Phytomedicine.2022, 96:153877.
  • ...
  • 生物活性
    Description: Piplartine shows potential anti-malaria, anti- leishmaniasis, anticancer, and mutagenic activities, it shows inhibitory activities of platelet aggregation induced by ADP and AA in vitro .
    Targets: P450 (e.g. CYP17) | Antifection
    In vitro:
    J Pharm Biomed Anal. 2014 Jul;95:113-20.
    In vitro metabolism of the alkaloid piplartine by rat liver microsomes.[Pubmed: 24667565]
    Because piplartine (PPT) has demonstrated biological activities, such as cytotoxic, anxiolytic, antidepressant, antifungal and antiplatelet activities, this molecule is a relevant drug candidate. The metabolic fate of drug candidates is an essential requirement in assessing their safety and efficacy. Based on this requirement, the biotransformation of PPT by cytochrome P450 enzymes (CYP) was investigated for the first time.
    METHODS AND RESULTS:
    To determine the in vitro enzymatic kinetic parameters, an HPLC method was developed and validated to quantify PPT. All samples were separated on a reversed-phase C18 column using a mobile phase of acetonitrile:water (40:60, v/v). The method exhibited a linear range of 2.4-157.7 μmol/L, with the following calibration curve: y=0.0934 (±0.0010)x+0.0027, r=0.9975. The lower limit of quantitation was verified to be 2.4 μmol/L, with an RSD below 7%. The precision and accuracy were assessed for both within-day and between-day determinations; neither relative standard (RSD%) deviations nor relative errors (RER) exceeded a value of 15%. The mean absolute recovery was 85%, with an RSD value below 6%. The enzymatic kinetic parameters revealed a sigmoidal profile, with V(max)=4.7±0.3 μmol/mg mL⁻¹/min, h=2.5±0.4, S₅₀=44.7±0.3 μmol/L and CL(max)=0.054 μL/min/mg protein, indicating cooperativity behavior. Employing a mammalian model, PPT metabolism yielded two unreported monohydroxylated products (m/z 334). The identification and structural elucidation of the metabolites were performed by comparing their mass spectra with those spectra of the parent drug.
    CONCLUSIONS:
    For the first time, the in vitro metabolism studies employing microsomes were demonstrated to be a suitable tool for data regarding enzymatic kinetics and for the metabolites formed in the PPT mammalian metabolism.
    Planta Med. 2015 Jan;81(1):15-9.
    Antitumour efficacy of Piper tuberculatum and piplartine based on the hollow fiber assay.[Pubmed: 25519832 ]
    Piper tuberculatum, popularly known in Brazil as "jaborandi falso" and "pimenta darta", is widely used in folk medicine for the treatment of several diseases.
    METHODS AND RESULTS:
    In this study, the in vivo hollow fiber assay was used to investigate the antitumour efficacy of the crude extract and piplartine obtained from P. tuberculatum roots. Human glioblastoma (SF-295) and colon carcinoma (HCT-8) cell lines were used. In vitro cytotoxicity was assayed by the MTT assay. In the hollow fiber assay, nude mice implanted with tumour cells in hollow fibers were treated for four consecutive days via the intraperitoneal route, and tumour cell populations were assessed by the MTT assay. Both the crude extract and piplartine displayed cytotoxicity. In the hollow fiber assay, tumour growth inhibition rates were 24.6-54.8 % for the crude extract and 33.7-62.2 % for piplartine. No signal of toxicity was noticed.
    CONCLUSIONS:
    In conclusion, the crude extract and piplartine obtained from P. tuberculatum roots displayed in vitro and in vivo anticancer efficacy.
    Chem Biol Drug Des. 2016 Jun;87(6):833-40.
    Design, Synthesis and Pharmacological Evaluation of Novel Piperlongumine derivatives as Potential Antiplatelet Aggregation Candidate.[Pubmed: 26706668 ]

    METHODS AND RESULTS:
    A series of novel piperlongumine derivatives (4a-i, 6a-i) were designed and synthesized. The inhibitory activities of platelet aggregation induced by ADP and AA in vitro have been evaluated by bron turbidimetry and liver microsomal incubated assay.
    CONCLUSIONS:
    The assay results show that compounds 4e and 6e exhibited remarkable potency to that of the positive control piplartine and aspirin.
    In vivo:
    Mutat Res. 2009 Jun-Jul;677(1-2):8-13.
    Piplartine induces genotoxicity in eukaryotic but not in prokaryotic model systems.[Pubmed: 19379832 ]
    Piplartine {5,6-dihydro-1-[(2E)-1-oxo-3-(3,4,5-trimethoxyphenyl)-2-propen-1-yl]-2(1H)-pyridinone} is an alkamide present in Piper species that exhibits promising anticancer properties. It was previously shown that piplartine is mutagenic in yeast and cultured mammalian cells.
    METHODS AND RESULTS:
    This study was performed to increase the knowledge on the mutagenic potential of piplartine using the Salmonella/microsome assay, V79 cell micronucleus and chromosome aberration assays, and mouse bone-marrow micronucleus tests. Piplartine was isolated from the roots of Piper tuberculatum. This extracted compound was unable to induce a mutagenic response in any Salmonella typhimurium strain either in the presence or absence of metabolic activation. Piplartine showed mutagenic effects in V79 cells, as there was an increased frequency of aberrant cells and micronuclei formation. In addition, piplartine administered at 50mg/kg did not induce micronucleus formation in vivo, but a dose of 100mg/kg induced an increase in the levels of micronucleus polychromatic erythrocytes (MNPCEs).
    CONCLUSIONS:
    Overall, these results provide further support that piplartine induces in vivo and in vitro mutagenicity in eukaryotic models.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.1516 mL 15.758 mL 31.5159 mL 63.0318 mL 78.7898 mL
    5 mM 0.6303 mL 3.1516 mL 6.3032 mL 12.6064 mL 15.758 mL
    10 mM 0.3152 mL 1.5758 mL 3.1516 mL 6.3032 mL 7.879 mL
    50 mM 0.063 mL 0.3152 mL 0.6303 mL 1.2606 mL 1.5758 mL
    100 mM 0.0315 mL 0.1576 mL 0.3152 mL 0.6303 mL 0.7879 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.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    Piperlotine A; Piperlotine A CFN96215 389572-70-7 C14H17NO2 = 231.3 5mg QQ客服:1413575084
    4'-Demethoxypiperlotine C; 4'-Demethoxypiperlotine C CFN96227 807372-38-9 C15H19NO3 = 261.3 5mg QQ客服:1413575084
    Piperlotine C; Piperlotine C CFN96220 886989-88-4 C16H21NO4 = 291.4 5mg QQ客服:1413575084
    Piperlotine D; Piperlotine D CFN96226 958296-13-4 C16H21NO4 = 291.4 5mg QQ客服:2056216494
    3-Phenyl-1-(pyrrol-1-yl)propan-1-one; 3-Phenyl-1-(pyrrol-1-yl)propan-1-one CFN96103 112448-69-8 C13H13NO = 199.3 5mg QQ客服:2056216494
    1-Cinnamoylpyrrole; 1-Cinnamoylpyrrole CFN96105 252248-89-8 C13H11NO = 197.2 5mg QQ客服:1457312923
    3-(4-Methoxyphenyl)-1-(pyrrol-1-yl)propan-1-one; 3-(4-Methoxyphenyl)-1-(pyrrol-1-yl)propan-1-one CFN96104 448905-82-6 C14H15NO2 = 229.3 5mg QQ客服:2056216494
    1-(4-Methoxycinnamoyl)pyrrole; 1-(4-Methoxycinnamoyl)pyrrole CFN96127 736140-70-8 C14H13NO2 = 227.3 5mg QQ客服:2056216494
    1-(3,4-Dimethoxycinnamoyl)piperidine; 1-(3,4-Dimethoxycinnamoyl)piperidine CFN96136 128261-84-7 C16H21NO3 = 275.4 5mg QQ客服:1457312923
    3'-二甲氧基荜茇明碱; 3'-Demethoxypiplartine CFN96121 130263-10-4 C16H17NO4 = 287.3 5mg QQ客服:2056216494

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