IB-MECA
中文名称:
IB-MECA
中文同义词:
N6-(3-碘苄基)腺苷-5-N-甲基糖酰胺;腺苷A3受体激动剂(IB-MECA)
英文名称:
IB-MECA
英文同义词:
PICLIDENOSON;CF-101;(2S,3S,4R,5R)-3,4-dihydroxy-5-(6-(3-iodobenzylamino)-9H-purin-9-yl)-N-methyltetrahydrofuran-2-carboxamide;CS-2564;IBMECA;(PICLIDENOSON; CF-101;1-DEOXY-1-[6-[[(3-IODOPHENYL)METHYL]AMINO]-9H-PURIN-9-YL]-N-METHYL-BETA-D-RIBOFURANURON-AMIDE;Selepressin;RPR-113090;3-iodobenzyl-5-N-methylcarboxamidoadenosine
CAS号:
152918-18-8
分子式:
C18H19IN6O4
分子量:
510.29
EINECS号:
相关类别:
细胞生物学试剂
Mol文件:
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
形态
solid
酸度系数(pKa)
12.72±0.70(Predicted)
颜色
white
InChIKey
HUJXGQILHAUCCV-MOROJQBDSA-N
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.
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.
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.
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.
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.
安全说明
22-24/25
WGK Germany
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