生物活性 靶点 体外研究 体内研究
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IB-MECA

生物活性 靶点 体外研究 体内研究
IB-MECA,152918-18-8,结构式
IB-MECA
  • CAS号:152918-18-8
  • 英文名:IB-MECA
  • 中文名:IB-MECA
  • CBNumber:CB5181025
  • 分子式:C18H19IN6O4
  • 分子量:510.29
  • MOL File:152918-18-8.mol
IB-MECA化学性质
  • 密度 :1.98±0.1 g/cm3(Predicted)
  • 储存条件 :2-8°C
  • 溶解度 :hot ethanol: >10 mg/mL
  • 酸度系数(pKa) :12.72±0.70(Predicted)
  • 形态 :solid
  • 颜色 :white
  • InChIKey :HUJXGQILHAUCCV-MOROJQBDSA-N
安全信息

IB-MECA性质、用途与生产工艺

  • 生物活性 Piclidenoson (IB-MECA) 是一种首创的，具有口服活性的，选择性的腺苷 A3 受体 (A3AR) 激动剂。Piclidenoson 在不同类型的癌细胞如黑色素瘤、白血病中表现出抗增殖和诱导凋亡 (apoptosis) 的作用。Piclidenoson 可用于自身免疫性炎症疾病和 COVID-19 的研究。
  • 靶点

    A3AR

  • 体外研究

    Piclidenoson is able to inhibit Forskolin (HY-15371)-stimulated cAMP levels with EC 50 s of 0.82 μM and 1.2 μM in OVCAR-3 cells and Caov-4 cells, respectively.
    Piclidenoson (0.0001-100 μM; 48 hours) significantly reduces cell viability in a dose-dependent manner in human ovarian cancer cell lines, with IC 50 s of 32.14 μM and 45.37 μM for OVCAR-3 and Caov-4 cells, respectively.
    Piclidenoson (0.001-100 μM; 48 hours) induces apoptosis in ovarian cancer cell line through the caspase pathway.
    Piclidenoson induces apoptosis via the mitochondrial signaling pathway.

    Cell Proliferation Assay

    Cell Line: OVCAR-3 cells, Caov-4 cells
    Concentration: 0.0001-100 μM
    Incubation Time: 48 hours
    Result: Resulted in a dose-dependent reduction in the cell viability.

    Apoptosis Analysis

    Cell Line: OVCAR-3 cells, Caov-4 cells
    Concentration: 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
    Incubation Time: 48 hours
    Result: Significant increased in the percentage of apoptosis in a concentration-dependent manner.

    Western Blot Analysis

    Cell Line: OVCAR-3 cells, Caov-4 cells
    Concentration: 1 μM, 10 μM, 100 μM
    Incubation Time: 48 hours
    Result: Decreased the expression of Bcl-2 was noticeably and increased the expression of Bax protein.
  • 体内研究

    Piclidenoson (105 μg/kg; i.p.) enhances survival of γ-irradiated mice.

    Animal Model: B10CBAF1 male mice aged 3 months (average 30 g)
    Dosage: 105 μg/kg
    Administration: Intraperitoneal injection, 0.5 h after irradiation
    Result: Resulted in statistically significant increases of the mean survival time in comparison with the control irradiated mice.
  • 用途  一种腺苷A3受体激动剂, EC50值为0.11μM。Piclidenoson is a specific agonist to the A3 adenosine receptor, which inhibits the development of colon carcinoma growth in cell cultures and xenograft murine models. CF101 has been shown to downregulate PKB/Akt and NF-κB protein expression level. CF101 potentiates the cytotoxic effect of 5-FU, thus preventing drug resistance. The myeloprotective effect of CF101 suggests its development as an add-on treatment to 5-FU.
IB-MECA上下游产品信息
上游原料
下游产品
IB-MECA生产厂家
  • 公司名称：Hangzhou Sage Chemical Co., Ltd.
  • 联系电话：+86057186818502 13588463833
  • 电子邮件：info@sagechem.com
  • 国家：中国
  • 产品数：10266
  • 优势度：58
  • 公司名称：成都诺维生物科技有限公司
  • 联系电话：028-81458053
  • 电子邮件：novibiotech@163.com sales@novi-biotech.com
  • 国家：中国
  • 产品数：226
  • 优势度：55
  • 公司名称：AdooQ BioScience, LLC
  • 联系电话：+1 (866) 930-6790
  • 电子邮件：info@adooq.com
  • 国家：美国
  • 产品数：2782
  • 优势度：58
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