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
- 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
- 安全说明 :22-24/25
- WGK Germany :3
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.
- 公司名称：SIGMA
- 联系电话：--
- 电子邮件：
- 国家：瑞士
- 产品数：6896
- 优势度：91
