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  • 蟾毒灵

    Bufalin

    蟾毒灵
    产品编号 CFN99947
    CAS编号 465-21-4
    分子式 = 分子量 C24H34O4 = 386.52
    产品纯度 >=98%
    物理属性 White powder
    化合物类型 Steroids
    植物来源 The glandular body of Bufo bufo gargarizans Cantor.
    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
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    蟾毒灵 CFN99947 465-21-4 10mg QQ客服:2159513211
    蟾毒灵 CFN99947 465-21-4 20mg QQ客服:2159513211
    蟾毒灵 CFN99947 465-21-4 50mg QQ客服:2159513211
    蟾毒灵 CFN99947 465-21-4 100mg QQ客服:2159513211
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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
  • Worcester Polytechnic Institute (USA)
  • Calcutta University (India)
  • Shanghai Institute of Organic Chemistry (China)
  • University of Cincinnati (USA)
  • University of Otago (New Zealand)
  • Leibniz-Institut für Pflanzenbiochemie (IPB) (Germany)
  • Georgia Institute of Technology (USA)
  • University of Malaya (Malaysia)
  • Uniwersytet Jagielloński w Krakowie (Poland)
  • University of Virginia (USA)
  • Chungnam National University (Korea)
  • University of Dicle (Turkey)
  • Medical University of Gdansk (Poland)
  • National Research Council of Canada (Canada)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Processes2020, 8(12),1540.
  • Biochem Biophys Res Commun.2020, 522(4):1052-1058
  • Biochem Biophys Res Commun.2018, 505(4):1148-1153
  • FASEB J.2022, 36(7):e22387.
  • Horticulture Research2020, 7:111.
  • Food Res Int.2019, 123:125-134
  • Appl. Sci.2020, 10(16),5482.
  • Journal of Analytical Chemistry2017, 854-861
  • Korean J. Medicinal Crop Sci.2022, 30(2):117-123.
  • FEMS Microbiol Lett.2017, 364(11)
  • Journal of Functional Foods2022, 96: 105216.
  • FEBS Lett.2021, 595(20):2608-2615.
  • Sci Rep.2016, 6:25094
  • Int J Mol Sci.2021, 22(19):10405.
  • Plants (Basel).2021, 10(12):2795.
  • Dent Mater J.2020, 39(4):690-695
  • Phytomedicine.2022, 100:154058.
  • J Med Food.2021, 24(2):151-160.
  • Nat Prod Sci.2019, 25(3):238
  • J of the Korean Society of Food Science and Nutrition2019, 32(2):148-154
  • J Asian Nat Prod Res.2019, 5:1-17
  • Plant Pathology2022, 13527
  • Journal of Apiculture2019, 34(2):131-136
  • ...
  • 生物活性
    Description: Bufalin a major digoxin-like immunoreactive component of the Chinese medicine Chan Su; has been shown to exert a potential for anticancer activity against various human cancer cell lines in vitro. Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators steroid receptor coactivator (SRC)-3 and SRC-1, it also as a potentially broad-spectrum small-molecule inhibitor for cancer. Bufalin can partly reverse the MDR of K562/VCR cells, with a possible mechanism of down-regulating MRP1 expression and activating apoptosis pathway by altering Bcl-xL/Bax ratio.
    Targets: PKA | cAMP | p38MAPK | Bcl-2/Bax | P-gp | Src | Akt
    In vitro:
    J Tradit Chin Med. 2014 Dec;34(6):678-83.
    Reversal effect of bufalin on multidrug resistance in K562/VCR vincristine-resistant leukemia cell line.[Pubmed: 25618972]
    To probe insights into the reversal effect of Bufalin on vincristine-acquired multidrug resistance (MDR) in human leukemia cell line K562/VCR.
    METHODS AND RESULTS:
    Proliferative inhibition rate and the reversal index (RI) of Bufalin were determined by Methyl thiazolyl tetrazolium assay. The uptake of Adriamycin (ADM) in K562/VCR cells, cell cycle and apoptosis rate were determined by flow cytometry (FCM). Cell morphologic changes were observed with Wright-Giemsa staining. The expression of P-glycoprotein (P-gp), multidrug-associated protein-1 (MRP1), Bcl-xL and Bax protein were measured by immunocytochemistry. The human leukemia multidrug resistant K562/VCR cells showed no cross-resistance to Bufalin. The RIs of Bufalin at concentrations of 0.0002, 0.001 and 0.005 μmol/L were 4.85, 6.94 and 14.77, respectively. Preincubation of 0.001 μmol/L Bufalin for 2 h could increase intracellular ADM fluorescence intensity to 28.07% (P < 0.05) and down-regulate MRP1 expression simultaneously, but no remarkable effect was found on P-gp protein. Cell cycle analysis indicated increased apoptosis rate and apparent decreased G2/M phase proportion after treatment with Bufalin. When exposed to 0.01 μmol/L Bufalin, typical morphological changes of apoptosis could be observed. Down-regulation of Bcl-xL and up-regulation of Bax expression in K562/VCR cells could be detected by immunocytochemistry.
    CONCLUSIONS:
    Bufalin could partly reverse the MDR of K562/VCR cells, with a possible mechanism of down-regulating MRP1 expression and activating apoptosis pathway by altering Bcl-xL/Bax ratio.
    J Biol Chem. 1996 Jun 14;271(24):14067-72.
    The cooperative interaction of two different signaling pathways in response to bufalin induces apoptosis in human leukemia U937 cells.[Pubmed: 8662906]
    Bufalin, an active principle of Chinese medicine, chan'su, induced typical apoptosis in human leukemia U937 cells.
    METHODS AND RESULTS:
    When U937 cells were treated with 10(-8) M Bufalin in the absence of serum, mitogen-activated protein (MAP) kinase activity was markedly increased 6 h after the start of treatment and elevated so for 12 h. Prior to the activation of MAP kinase, increased activities of Ras, Raf-1, and MAP kinase kinase were found, but these enzymes were transiently activated by the treatment with Bufalin. These results suggest that the signal was transmitted sequentially from Ras, Raf-1, and MAP kinase kinase to MAP kinase. In association with this signal transduction, the concentration of cAMP in the cells decreased markedly, suggesting that Raf-1 was also activated by a decrease in the extent of phosphorylation by protein kinase A. In fact, pretreatment of U937 cells with forskolin and 3-isobutyl-1-methylxanthine, which are known to increase the concentration of cAMP in the cells, and subsequent treatment with Bufalin resulted in a decrease in both Raf-1 activity and DNA fragmentation. To confirm the participation of MAP kinase in the apoptotic process, antisense cDNA for MAP kinase kinase 1 was expressed in U937 cells. The transformants were significantly resistant to both DNA fragmentation and cell death in response to Bufalin.
    CONCLUSIONS:
    Our findings suggest that a pathway with the persistent activation of MAP kinase in U937 cells in response to Bufalin is at least one of the signal transduction pathways involved in the induction of apoptosis.
    In vivo:
    Environ Toxicol . 2017 Apr;32(4):1305-1317.
    Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo[Pubmed: 27444971]
    Abstract Bufalin has been shown to be effective against a variety of cancer cells, but its role in lung cancer has never been studied in an animal model. In this study, we evaluated bufalin effects in a human lung cancer cell line NCI-H460 both in vitro and in vivo. Bufalin caused significant cytotoxicity in NCI-H460 cells at a concentration as low as 1 μM. DNA condensation was observed in bufalin-treated cells in a dose-dependent manner. Mitochondrial membrane potential (ΔΨm ) was reduced and reactive oxygen species (ROS) were increased in bufalin-treated NCI-H460 cells. Levels of several proapoptotic proteins such as Fas, Fas-ligand, cytochrome c, apoptosis protease activating factor-1, endonuclease G, caspase-3 and caspase-9 were increased after bufalin treatment. At the same time, anti-apoptotic B-cell lymphoma 2 protein levels were reduced. Bufalin decreased glucose regulated protein-78 gene expression but increased growth arrest- and DNA damage-inducible 153 gene expression. Bufalin injected intraperitoneally in a dose-dependent manner reduced tumor size in BALB/C nu/nu mice implanted with NCI-H460 cells. Bufalin injection did not produce significant drug-related toxicity in experimental animals except at a high dose (0.4 mg kg-1 ). In conclusion, low concentrations of bufalin can induce apoptosis in the human lung cancer cell line NCI-H460 in vitro. Bufalin also reduced tumor size in mice injected with NCI-H460 cells without significant drug-related toxicity. These results indicate that bufalin may have potential to be developed as an agent for treating human non-small cell lung cancer. © 2016 Wiley Periodicals, Inc. Environ Toxicol 32: 1305-1317, 2017. Keywords: animal models; apoptosis; bufalin; lung neoplasm.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.5872 mL 12.9359 mL 25.8719 mL 51.7438 mL 64.6797 mL
    5 mM 0.5174 mL 2.5872 mL 5.1744 mL 10.3488 mL 12.9359 mL
    10 mM 0.2587 mL 1.2936 mL 2.5872 mL 5.1744 mL 6.468 mL
    50 mM 0.0517 mL 0.2587 mL 0.5174 mL 1.0349 mL 1.2936 mL
    100 mM 0.0259 mL 0.1294 mL 0.2587 mL 0.5174 mL 0.6468 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
    19-羟基蟾毒灵; 19-Hydroxybufalin CFN91020 39844-86-5 C24H34O5 = 402.52 5mg QQ客服:2159513211
    远华蟾蜍精; Telocinobufagin CFN90213 472-26-4 C24H34O5 = 402.52 20mg QQ客服:2159513211
    嚏根草醇; Hellebrigenol CFN91021 508-79-2 C24H34O6 = 418.52 5mg QQ客服:3257982914
    日本蟾蜍毒苷元; Gamabufotalin CFN90212 465-11-2 C24H34O5 = 402.52 20mg QQ客服:2159513211
    沙蟾毒精; Arenobufagin CFN98578 464-74-4 C24H32O6 = 416.51 20mg QQ客服:3257982914
    伪异沙蟾毒精; Bufarenogin CFN90151 17008-65-0 C24H32O6 = 416.51 5mg QQ客服:2056216494
    伪异沙蟾毒精; Pseudobufarenogin CFN91017 17008-69-4 C24H32O6 = 416.51 10mg QQ客服:2159513211
    蟾毒它灵, 蟾蜍他灵; Bufotaline CFN98545 471-95-4 C26H36O6 = 444.56 20mg QQ客服:1413575084
    酯蟾毒配基,蟾力苏; Resibufogenin CFN98543 465-39-4 C24H32O4 = 384.51 20mg QQ客服:3257982914
    酯蟾毒精; Resibufagin CFN91013 20987-24-0 C24H30O5 = 398.49 5mg QQ客服:1413575084

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