152918-18-8

中文名称 IB-MECA

英文名称 IB-MECA

CAS 152918-18-8

分子式 C18H19IN6O4

分子量 510.29

MOL 文件 152918-18-8.mol

152918-18-8 结构式

基本信息物理化学性质应用领域安全数据常见问题列表

基本信息

中文别名

腺苷A3受体激动剂(IB-MECA)
N6-(3-碘苄基)腺苷-5'-N-甲基糖酰胺

英文别名

CF-101
CS-2564
IB-MECA
RPR-113090
Selepressin
PICLIDENOSON
CF-101
Piclidenoson (IB-MECA)
IBMECA
(PICLIDENOSON
CF-101
IB-MECA SELECTIVE A3 ADENOSIN
N6-(3-IODOBENZYL)ADO-5'N-METHYLURONAMIDE

所属类别

生物化工：激动剂抑制剂

物理化学性质

密度1.98±0.1 g/cm3(Predicted)

储存条件2-8°C

溶解度hot ethanol: >10 mg/mL

溶解度热乙醇：>10 mg/mL

酸度系数(pKa)12.72±0.70(Predicted)

形态solid

颜色white

InChIKeyHUJXGQILHAUCCV-MOROJQBDSA-N

应用领域

用途1

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.

安全数据

安全说明22-24/25

WGK Germany3

常见问题列表

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.