IB-MECA

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);化合物PICLIDENOSON;(2S,3S,4R,5R)-3,4-二羟基-5-(6-((3-碘苄基)氨基)-9H-嘌呤-9-基)-N-甲基四氢呋喃-2-甲酰胺;PICLIDENOSON IB-MECA; CF-101;IB-MECA,A 3激动剂
英文名称IB-MECA
英文同义词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;IB-MECA;N6-(3-IODOBENZYL)ADO-5'N-METHYLURONAMIDE;n(6)-(3-iodobenzyl)-5’-n-methylcarboxamidoadenosine;IB-MECA SELECTIVE A3 ADENOSIN
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;医药原料
Mol文件152918-18-8.mol
结构式IB-MECA 结构式

IB-MECA 性质

密度1.98±0.1 g/cm3(Predicted)
储存条件2-8°C
溶解度热乙醇:>10 mg/mL
酸度系数(pKa)12.72±0.70(Predicted)
形态固体
颜色白色
InChIKeyHUJXGQILHAUCCV-MOROJQBDSA-N

IB-MECA 用途与合成方法

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。

A3AR

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.

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.

安全信息

安全说明22-24/25
WGK Germany3

MSDS信息

提供商 语言
英文

IB-MECA 上下游产品信息

"IB-MECA"相关产品信息
(S)-(+)-四氢糠胺
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