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  • 苦龙胆脂甙

    Amarogentin

    苦龙胆脂甙
    产品编号 CFN90519
    CAS编号 21018-84-8
    分子式 = 分子量 C29H30O13 = 586.54
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Iridoids
    植物来源 The roots of Gentiana scabra Bunge
    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
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    苦龙胆脂甙 CFN90519 21018-84-8 10mg QQ客服:215959384
    苦龙胆脂甙 CFN90519 21018-84-8 20mg QQ客服:215959384
    苦龙胆脂甙 CFN90519 21018-84-8 50mg QQ客服:215959384
    苦龙胆脂甙 CFN90519 21018-84-8 100mg QQ客服:215959384
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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
  • University of Toronto (Canada)
  • Mahatma Gandhi University (India)
  • Universidade Federal de Goias (UFG) (Brazil)
  • Universidade Federal de Pernambuco (UFPE) (Brazil)
  • Almansora University (Egypt)
  • University of Beira Interior (Portugal)
  • Northeast Normal University Changchun (China)
  • Worcester Polytechnic Institute (USA)
  • Yale University (USA)
  • Warszawski Uniwersytet Medyczny (Poland)
  • Harvard University (USA)
  • Deutsches Krebsforschungszentrum (Germany)
  • Sant Gadge Baba Amravati University (India)
  • Funda??o Universitária de Desenvolvimento (Brazil)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Plants (Basel).2021, 10(11):2317.
  • Carbohydrate Polymer Technologies & App.2021, 2:100049.
  • Front Microbiol.2019, 10:2806
  • Plant Biotechnology Reports 2021, 15:117-124.
  • Turk J Med Sci.2023 53: 1312-1320.
  • Arch Pharm Res.2015, 38(6):1080-9
  • Front Pharmacol.2023, 14:1244655.
  • Daru.2022, 30(2):273-288.
  • Plant Growth Regulation2020, 90(2):383-392
  • Proc Natl Acad Sci USA.2016, 113(30):E4407-1
  • Biochem Biophys Res Commun.2020, 527(4):889-895.
  • Molecules.2017, 22(3)
  • New Zealand J. Forestry Sci.2014, 44:17
  • Phytomedicine.2021, 83:153483.
  • Chem Biol Interact.2020, 328:109200.
  • Food Chem.2021, 377:131976.
  • Planta Med.2023, a-2192-2281.
  • PLoS One.2018, 13(3):e0193386
  • Sci Rep.2023, 13(1):14594.
  • Oncotarget.2015, 6(31):30831-49
  • Molecules.2021, 26(18):5665.
  • Drug Des Devel Ther.2020, 14:969-976.
  • Antioxidants.2022, 11(4), 67.
  • ...
  • 生物活性
    Description: Amarogentin incorporated in liposomes or niosomes may have clinical application in the treatment of leishmaniasis. It plays cemopreventive/therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis. Amarogentin may offer therapeutic potential for preventing or treating thromboembolic disorders, it prevents platelet activation through the inhibition of PLC γ2-PKC cascade and MAPK pathway.
    Targets: COX | PKC | MAPK | p53 | p21 | Caspase | Bcl-2/Bax | PARP | c-Myc
    In vitro:
    PLoS One. 2014 Mar 6;9(6):e90637.
    The bitter barricading of prostaglandin biosynthesis pathway: understanding the molecular mechanism of selective cyclooxygenase-2 inhibition by amarogentin, a secoiridoid glycoside from Swertia chirayita.[Pubmed: 24603686]
    Amarogentin, a bitter secoiridoid glycoside from S. chirayita, shows varied activity in several patho-physiological conditions, predominantly in leishmaniasis and carcinogenesis. Experimental analysis has revealed that Amarogentin downregulates the cyclooxygenase-2 (COX-2) activity and helps to curtail skin carcinogenesis in mouse models; however, there exists no account on selective inhibition of the inducible cyclooxygenase (COX) isoform by Amarogentin.
    METHODS AND RESULTS:
    Hence the computer-aided drug discovery methods were used to unravel the COX-2 inhibitory mechanism of Amarogentin and to check its selectivity for the inducible isoform over the constitutive one. The generated theoretical models of both isoforms were subjected to molecular docking analysis with Amarogentin and twenty-one other Food and Drug Authority (FDA) approved lead molecules. The post-docking binding energy profile of Amarogentin was comparable to the binding energy profiles of the FDA approved selective COX-2 inhibitors. Subsequent molecular dynamics simulation analysis delineated the difference in the stability of both complexes, with Amarogentin-COX-2 complex being more stable after 40ns simulation. The total binding free energy calculated by MMGBSA for the Amarogentin-COX-2 complex was -52.35 KCal/mol against a binding free energy of -8.57 KCal/mol for Amarogentin-COX-1 complex, suggesting a possible selective inhibition of the COX-2 protein by the natural inhibitor. Amarogentin achieves this potential selectivity by small, yet significant, structural differences inherent to the binding cavities of the two isoforms. Hypothetically, it might block the entry of the natural substrates in the hydrophobic binding channel of the COX-2, inhibiting the cyclooxygenation step.
    CONCLUSIONS:
    To sum up briefly, this work highlights the mechanism of the possible selective COX-2 inhibition by Amarogentin and endorses the possibility of obtaining efficient, futuristic and targeted therapeutic agents for relieving inflammation and malignancy from this phytochemical source.
    J Antimicrob Chemother. 1999 Dec;44(6):791-4.
    Evaluation of the in-vivo activity and toxicity of amarogentin, an antileishmanial agent, in both liposomal and niosomal forms.[Pubmed: 10590280]

    METHODS AND RESULTS:
    The antileishmanial property of amarogentin, a secoiridoid glycoside isolated from the Indian medicinal plant Swertia chirata, was examined in a hamster model of experimental leishmaniasis. The therapeutic efficacy of amarogentin was evaluated in free and two different vesicular forms, liposomes and niosomes. The amarogentin in both liposomal and niosomal forms was found to be a more active leishmanicidal agent than the free amarogentin; and the niosomal form was found to be more efficacious than the liposomal form at the same membrane microviscosity level. Toxicity studies involving blood pathology, histological staining of tissues and specific enzyme levels related to normal liver function showed no toxicity.
    CONCLUSIONS:
    Hence, amarogentin incorporated in liposomes or niosomes may have clinical application in the treatment of leishmaniasis.
    In vivo:
    Biomed Res Int. 2014;2014:728019.
    Amarogentin, a secoiridoid glycoside, abrogates platelet activation through PLC γ 2-PKC and MAPK pathways.[Pubmed: 24868545]
    Amarogentin, an active principle of Gentiana lutea, possess antitumorigenic, antidiabetic, and antioxidative properties. Activation of platelets is associated with intravascular thrombosis and cardiovascular diseases.
    METHODS AND RESULTS:
    The present study examined the effects of amarogentin on platelet activation. Amarogentin treatment (15~60  μM) inhibited platelet aggregation induced by collagen, but not thrombin, arachidonic acid, and U46619. Amarogentin inhibited collagen-induced phosphorylation of phospholipase C (PLC) γ2, protein kinase C (PKC), and mitogen-activated protein kinases (MAPKs). It also inhibits in vivo thrombus formation in mice. In addition, neither the guanylate cyclase inhibitor ODQ nor the adenylate cyclase inhibitor SQ22536 affected the amarogentin-mediated inhibition of platelet aggregation, which suggests that amarogentin does not regulate the levels of cyclic AMP and cyclic GMP.
    CONCLUSIONS:
    In conclusion, amarogentin prevents platelet activation through the inhibition of PLC γ2-PKC cascade and MAPK pathway. Our findings suggest that amarogentin may offer therapeutic potential for preventing or treating thromboembolic disorders.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 1.7049 mL 8.5246 mL 17.0491 mL 34.0983 mL 42.6228 mL
    5 mM 0.341 mL 1.7049 mL 3.4098 mL 6.8197 mL 8.5246 mL
    10 mM 0.1705 mL 0.8525 mL 1.7049 mL 3.4098 mL 4.2623 mL
    50 mM 0.0341 mL 0.1705 mL 0.341 mL 0.682 mL 0.8525 mL
    100 mM 0.017 mL 0.0852 mL 0.1705 mL 0.341 mL 0.4262 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
    断马钱子酸; Secologanic acid CFN95028 60077-46-5 C16H22O10 = 374.3 20mg QQ客服:2159513211
    表断马钱子甙半缩醛内酯; Epivogeloside CFN99283 118627-52-4 C17H24O10 = 388.4 5mg QQ客服:3257982914
    断马钱子苷半缩醛内酯; Vogeloside CFN96444 60077-47-6 C17H24O10 = 388.37 5mg QQ客服:2159513211
    Gelidoside; Gelidoside CFN89019 128420-44-0 C35H42O21 = 798.7 10mg QQ客服:1457312923
    Trifloroside ; Trifloroside CFN96606 53823-10-2 C35H42O20 = 782.70 10mg QQ客服:215959384
    龙胆苦苷; Gentiopicroside CFN98047 20831-76-9 C16H20O9 = 356.3 20mg QQ客服:3257982914
    6'-O-β-D-葡萄糖基龙胆苦苷; 6'-O-beta-D-Glucosylgentiopicroside CFN90678 115713-06-9 C22H30O14 = 518.47 20mg QQ客服:2159513211
    獐牙菜苷; Sweroside CFN99455 14215-86-2 C16H22O9 = 358.3 20mg QQ客服:1413575084
    6'-O-β-D-芹糖獐芽菜苷; 6'-O-beta-D-Apiofuranosylsweroside CFN90752 266678-59-5 C21H30O13 = 490.5 5mg QQ客服:2056216494
    苦龙胆脂甙; Amarogentin CFN90519 21018-84-8 C29H30O13 = 586.54 20mg QQ客服:2056216494

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