1. 诱导疾病模型产品 NF-κB Apoptosis
  2. 消化系统疾病模型 生殖系统疾病模型 NF-κB Apoptosis
  3. 肝脏疾病模型
  4. Triptolide

Triptolide  (Synonyms: 雷公藤甲素; PG490)

目录号: HY-32735 纯度: 99.86%
COA 产品使用指南

Triptolide是从雷公藤根中提取的二萜类三环氧化物,具有免疫抑制,抗炎,抗增殖和抗肿瘤作用。 雷公藤内酯是 NF-κB 活化的抑制剂。

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Triptolide Chemical Structure

Triptolide Chemical Structure

CAS No. : 38748-32-2

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Customer Review

Other Forms of Triptolide:

MCE 顾客使用本产品发表的 43 篇科研文献

WB

    Triptolide purchased from MCE. Usage Cited in: Int J Mol Sci. 2016 Dec 19;17(12). pii: E2139.  [Abstract]

    To explore the cellular mechanisms for the suppression of CNE cells by TPL and IR, the expression of p65, phosph-p65, Bcl-2, and Bax in CNE cells are examined by Western blot, with β-actin as protein loading control. Western blot assay for Bax, Bcl-2, phosph-p65, and p65 expression in vitro with combined treatment with TPL and IR.

    查看 NF-κB 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor[1][2][3][4][5][6].

    IC50 & Target[1][2]

    HSP90

     

    MDM-2/p53

    47-73 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    786-0 IC50
    0.022 μM
    Compound: 1
    Cytotoxicity against human 786-O cells after 72 hrs by MTT assay
    Cytotoxicity against human 786-O cells after 72 hrs by MTT assay
    [PMID: 19637874]
    A549 IC50
    0.0175 μM
    Compound: Triptolide
    Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Cytotoxic activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 28011223]
    A549 IC50
    0.059 μM
    Compound: 1
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    A549 IC50
    14 nM
    Compound: 19
    Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay
    Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay
    [PMID: 23895492]
    A549 IC50
    23 nM
    Compound: 19
    Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA
    Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA
    [PMID: 23895492]
    B16-F10 IC50
    0.005 μM
    Compound: 1
    Antiproliferative activity against human B16-F10 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    Antiproliferative activity against human B16-F10 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    [PMID: 32028140]
    Bel-7402 IC50
    0.02 μM
    Compound: 1
    Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
    Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    BGC-823 IC50
    0.002 μM
    Compound: 1
    Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    Antiproliferative activity against human BGC-823 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    [PMID: 32028140]
    DU-145 IC50
    0.024 μM
    Compound: 1
    Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
    Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    HaCaT IC50
    0.027 μM
    Compound: TPL
    Cytotoxicity against human HaCaT cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human HaCaT cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    HCT-116 IC50
    0.003 μM
    Compound: 1
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    [PMID: 32028140]
    HCT-116 IC50
    0.01 μM
    Compound: 1
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    HCT-116 IC50
    0.046 μM
    Compound: TPL
    Cytotoxicity against human HCT-116 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    HCT-15 IC50
    0.029 μM
    Compound: 1
    Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
    Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    HeLa IC50
    0.043 μM
    Compound: TP
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    HeLa IC50
    0.047 μM
    Compound: 1
    Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
    Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
    [PMID: 19637874]
    Hepatocyte IC50
    37.7 nM
    Compound: TP
    Cytotoxicity against primary hepatocytes (unknown origin) after 48 hrs by XTT assay
    Cytotoxicity against primary hepatocytes (unknown origin) after 48 hrs by XTT assay
    [PMID: 30613335]
    HepG2 IC50
    0.014 μM
    Compound: 1
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    [PMID: 32028140]
    HepG2 IC50
    0.033 μM
    Compound: TP
    Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    HepG2 IC50
    0.468 μM
    Compound: Triptolide
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by CCK-8 assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by CCK-8 assay
    [PMID: 35476958]
    HepG2 IC50
    43.3 nM
    Compound: TP
    Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay
    Cytotoxicity against human HepG2 cells after 48 hrs by XTT assay
    [PMID: 30613335]
    HT-29 IC50
    0.047 μM
    Compound: TPL
    Cytotoxicity against human HT-29 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    HUVEC IC50
    0.044 μM
    Compound: TPL
    Cytotoxicity against HUVEC incubated for 72 hrs by MTT assay
    Cytotoxicity against HUVEC incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    K562 IC50
    0.05 μM
    Compound: 1
    Cytotoxicity against human K562 cells after 72 hrs by MTT assay
    Cytotoxicity against human K562 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    KB IC50
    0.043 μM
    Compound: 1
    Cytotoxicity against human KB cells after 72 hrs by MTT assay
    Cytotoxicity against human KB cells after 72 hrs by MTT assay
    [PMID: 19637874]
    KBM5 IC50
    10.3 nM
    Compound: 1
    Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay
    Cytotoxicity against human KBM5 cells harboring wild type Bcr-Abl after 72 hrs by MTS assay
    [PMID: 20149665]
    KBM5 IC50
    8.3 nM
    Compound: 1
    Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay
    Cytotoxicity against imatinib-resistant human KBM5 cells harboring Bcr-Abl T315I mutant after 72 hrs by MTS assay
    [PMID: 20149665]
    L02 IC50
    0.016 μM
    Compound: TPL
    Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    L02 IC50
    0.021 μM
    Compound: TP
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human HL7702 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    LNCaP IC50
    9.7 nM
    Compound: 1
    Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against androgen-sensitive human LNCaP cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    [PMID: 35247754]
    MCF7 IC50
    0.019 μM
    Compound: 1
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    MCF7 IC50
    0.022 μM
    Compound: TP
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    MDA-MB-231 IC50
    0.024 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    MDA-MB-231 IC50
    0.051 μM
    Compound: TPL
    Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    MDA-MB-468 IC50
    0.01 μM
    Compound: 1
    Cytotoxicity against human MDA-MB-468 cells by SRB assay
    Cytotoxicity against human MDA-MB-468 cells by SRB assay
    [PMID: 19637874]
    MEF IC50
    9200 nM
    Compound: 1
    Cytotoxicity against MEF after 72 hrs by MTS assay
    Cytotoxicity against MEF after 72 hrs by MTS assay
    [PMID: 20149665]
    MKN-28 IC50
    0.2 μM
    Compound: 1
    Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay
    Cytotoxicity against human MKN28 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    MOLT-4 IC50
    0.017 μM
    Compound: 1
    Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay
    Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    NCI-H1299 IC50
    0.049 μM
    Compound: TP
    Cytotoxicity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    NCI-H1650 IC50
    0.015 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell growth incubated for 96 hrs by MTT assay
    [PMID: 32028140]
    NCI-H1975 IC50
    0.002 μM
    Compound: TPL
    Cytotoxicity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    NCI-H1975 IC50
    0.019 μM
    Compound: TP
    Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    NCI-H460 IC50
    0.014 μM
    Compound: TPL
    Cytotoxicity against human NCI-H460 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    PANC-1 IC50
    0.056 μM
    Compound: TP
    Cytotoxicity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human PANC-1 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    PANC-1 IC50
    0.2 μM
    Compound: 8; TPL
    Cytotoxicity against human Panc-1 cells incubated for 48 hrs by CCK8 assay
    Cytotoxicity against human Panc-1 cells incubated for 48 hrs by CCK8 assay
    [PMID: 33289552]
    PC-3 IC50
    0.0183 μM
    Compound: Triptolide
    Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Cytotoxic activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 28011223]
    PC-3 IC50
    0.02 μM
    Compound: 1
    Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
    Antiproliferative activity against human PC3 cells after 72 hrs by SRB assay
    [PMID: 20833543]
    PC-3 IC50
    0.02 μM
    Compound: 1
    Cytotoxicity against human PC3 cells by SRB assay
    Cytotoxicity against human PC3 cells by SRB assay
    [PMID: 19637874]
    PC-3 IC50
    0.02 μM
    Compound: 1
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
    [PMID: 25467158]
    PC-3 IC50
    0.021 μM
    Compound: TP
    Cytotoxicity against human PC-3 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    Cytotoxicity against human PC-3 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
    [PMID: 34700239]
    PC-3 IC50
    0.043 μM
    Compound: 1
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    PC-3 IC50
    20 nM
    Compound: 1
    Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human PC3 cells after 72 hrs by sulforhodamine B assay
    [PMID: 24378709]
    PC-3 IC50
    20.3 nM
    Compound: 1
    Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    [PMID: 35247754]
    RAW264.7 IC50
    0.014 μM
    Compound: 1
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    [PMID: 32028140]
    RAW264.7 IC50
    0.023 μM
    Compound: 1
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 incubated for 1 hr followed by LPS stimulation and measured after 24 hrs by ELISA
    [PMID: 32028140]
    SGC-7901 IC50
    0.015 μM
    Compound: 1
    Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
    Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    SJRH30 IC50
    0.014 μM
    Compound: 1
    Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay
    Cytotoxicity against human Rh30 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    SK-OV-3 IC50
    0.006 μM
    Compound: 1
    Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay
    Antiproliferative activity against human SKOV3 cells after 72 hrs by SRB assay
    [PMID: 20833543]
    SK-OV-3 IC50
    0.0072 μM
    Compound: Triptolide
    Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Cytotoxic activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 28011223]
    SK-OV-3 IC50
    0.009 μM
    Compound: 1
    Cytotoxicity against human SKOV3 cells by SRB assay
    Cytotoxicity against human SKOV3 cells by SRB assay
    [PMID: 19637874]
    SK-OV-3 IC50
    0.01 μM
    Compound: 1
    Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
    Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    SK-OV-3 IC50
    6 nM
    Compound: 1
    Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human SKOV3 cells after 72 hrs by sulforhodamine B assay
    [PMID: 24378709]
    SMMC-7721 IC50
    0.018 μM
    Compound: 1
    Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
    Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    SW 1116 IC50
    0.052 μM
    Compound: 1
    Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay
    Cytotoxicity against human SW1116 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    SW480 IC50
    50 nM
    Compound: 77
    Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay
    [PMID: 33445154]
    SW-620 IC50
    0.163 μM
    Compound: TPL
    Cytotoxicity against human SW-620 cells incubated for 72 hrs by MTT assay
    Cytotoxicity against human SW-620 cells incubated for 72 hrs by MTT assay
    [PMID: 35617856]
    U-251 IC50
    0.033 μM
    Compound: 1
    Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
    Cytotoxicity against human U251 cells assessed as inhibition of cell proliferation by sulforhodamine B assay
    [PMID: 25467158]
    U-251 IC50
    0.049 μM
    Compound: 1
    Cytotoxicity against human U251 cells after 72 hrs by MTT assay
    Cytotoxicity against human U251 cells after 72 hrs by MTT assay
    [PMID: 19637874]
    体外研究
    (In Vitro)

    Triptolide 在培养的和原发性慢性淋巴细胞白血病 (CLL) B 细胞中诱导细胞凋亡。用 Triptolide 处理 CD19+ B 细胞,诱导培养的和原代 CLL 细胞凋亡的剂量依赖性增加。Triptolide 对高风险 (n=5) 和低风险 CLL (n=12) B 细胞 (10-50 nM 范围) 具有选择性毒性,同时在很大程度上保留正常 B 细胞 (n=5)。与抑制热休克诱导的 HSP 转录一致,Triptolide 处理可减弱热休克诱导的 HSP 表达[1]
    Triptolide 是一种源自中国植物雷公藤的天然产物,据报道在多种癌症中表现出抗肿瘤作用。Triptolide 以剂量依赖性方式抑制 MDM2 表达,即使在 20-100 nM 的低浓度下,在急性淋巴细胞白血病 (ALL) 细胞中也是如此。Triptolide 在所有 8 种具有天然 MDM2 过表达的细胞系中表现出强烈的细胞毒活性,IC50 值范围为 47 到 73 nM。雷公藤甲素对表达极低水平 MDM2 的 EU-4 细胞的细胞毒性作用要小得多,而当 MDM2 稳定转染时,雷公藤甲素能有效杀死这些细胞 (IC50 值:725 nM 对 88 nM)[2]
    分化的 PC12 细胞与不同浓度的 Triptolide (0.01、0.1 和1 nM) 在10 μM Aβ25-35 存在下孵育 24 小时,MTT 法检测雷公藤甲素的作用.结果表明,Aβ25-35可降低细胞活力,Triptolide 处理后分化的PC12细胞活力显著增加。结果表明雷公藤甲素可以减轻 Aβ25-35引起的细胞损伤,说明雷公藤甲素具有神经保护作用[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    小鼠接受静脉注射后 Triptolide (TP) 血浆浓度迅速下降。注射 2 小时后,所有三组的 Triptolide 浓度均降至低于定量下限。在对照组和处理组之间进行参数比较,以评估 P-gp 抑制对 Triptolide 暴露和消除的影响。mdr1a-siRNA处理可显著增加雷公藤甲素血浆暴露,Cmax从 413±74 增加到510±94 ng/mL (P<0.05),AUC 从 103.5±9.6 增加到 154.3±30.2 ng h/mL (P<0.05)。在 Tariquidar 的伴随组中,还注意到显著增加的 AUC,从对照的 103.5±9.6 到 Triptolide + Tariquidar 组的 145.9±24.6 ng h/mL。因此,雷公藤甲素在小鼠体内的总体清除率显著降低,从对照组的 9564±1024.2 mL/min/kg 降至对照组的 6576.4±1438.5 (P<0.05) 和对照组的 5755.4±1200.1 mL/min/kg (P<0.05) 分别为雷公藤甲素+Tariquidar和雷公藤甲素+mdr1a-siRNA组[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    360.40

    Formula

    C20H24O6

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    雷公藤甲素;雷藤素甲;雷公藤内酯醇;雷公藤多甙

    结构分类
    初始来源
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 25 mg/mL (69.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7747 mL 13.8735 mL 27.7469 mL
    5 mM 0.5549 mL 2.7747 mL 5.5494 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.17 mg/mL (3.25 mM); 澄清溶液

      此方案可获得 ≥ 1.17 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 11.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.17 mg/mL (3.25 mM); 澄清溶液

      此方案可获得 ≥ 1.17 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 11.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.86%

    参考文献
    Cell Assay
    [3]

    The viability of differentiated PC12 cells treated with different concentrations of Triptolide. After differentiated PC12 cells are cultured on 96-well plates with RPMI 1640 medium for stabilization, differentiated PC12 cells are incubated with different concentrations of Triptolide (0.01, 0.1, and 1 nM) for 24 hours. The concentrations in this study are chosen. Then cell viability is determined by the MTT assay. Each condition and experiment is repeated three times[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    Mice[4]
    Male BALB/C mice (weight, 18-22 g) are used. For Triptolide (TP) plasma kinetic study and toxicological evaluation, mice are divided into four groups (n=5 each) to collect blood and tissue samples: (1) normal+saline group; (2) 1.0 mg/kg Triptolide+15 nmol negative control (NC) siRNA-siRNA group; (3) 1.0 mg/kg Triptolide+15 nmol mdr1a-siRNA group; (4) 1.0 mg/kg Triptolide+10 mg/kg Tariquidar group. In order to avoid the complication caused by drug absorption or possible intestinal first-pass effect, Triptolide and the inhibitor are intravenously administrated to mice. The siRNA group is intravenously injected with NC-siRNA or mdr1a-siRNA 2 days before Triptolide dose. For Triptolide+Tariquidar group, the mice are received an intravenous Tariquidar dose 20 min prior to the Triptolide injection. Blood samples are collected at 2, 5, 10, 15, 30, 60 and 120 min after Triptolide dosing. To assess the liver exposure of Triptolide, liver tissue samples are collected from another set of mice at 5, 30, 60 and 120 min after dosing. Three Triptolide groups are design for this experiment, including Triptolide+NC-siRNA group, Triptolide+mdr1a-siRNA group and Triptolide+Tariquidar group. The liver tissue samples are weighed and then homogenized in 10 volume (w:v) of ice-cold saline. The concentrations of Triptolide in plasma and liver tissue are measured by a validated LC-MS/MS method.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7747 mL 13.8735 mL 27.7469 mL 69.3674 mL
    5 mM 0.5549 mL 2.7747 mL 5.5494 mL 13.8735 mL
    10 mM 0.2775 mL 1.3873 mL 2.7747 mL 6.9367 mL
    15 mM 0.1850 mL 0.9249 mL 1.8498 mL 4.6245 mL
    20 mM 0.1387 mL 0.6937 mL 1.3873 mL 3.4684 mL
    25 mM 0.1110 mL 0.5549 mL 1.1099 mL 2.7747 mL
    30 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
    40 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7342 mL
    50 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
    60 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    Triptolide
    目录号:
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