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152918-18-8

中文名稱 IB-MECA
英文名稱 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 結(jié)構(gòu)式 152918-18-8 結(jié)構(gòu)式

基本信息

中文別名
腺苷A3受體激動劑(IB-MECA)
N6-(3-碘芐基)腺苷-5'-N-甲基糖酰胺
英文別名
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
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

密度1.98±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度hot ethanol: >10 mg/mL
溶解度熱乙醇:>10 mg/mL
酸度系數(shù)(pKa)12.72±0.70(Predicted)
形態(tài)solid
顏色white
InChIKeyHUJXGQILHAUCCV-MOROJQBDSA-N

應(yīng)用領(lǐng)域

用途1
一種腺苷A3受體激動劑, EC50值為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.

安全數(shù)據(jù)

安全說明22-24/25
WGK Germany3
WGK Germany3

常見問題列表

生物活性
Piclidenoson (IB-MECA) 是一種首創(chuàng)的,具有口服活性的,選擇性的腺苷 A3 受體 (A3AR) 激動劑。Piclidenoson 在不同類型的癌細胞如黑色素瘤、白血病中表現(xiàn)出抗增殖和誘導(dǎo)凋亡 (apoptosis) 的作用。Piclidenoson 可用于自身免疫性炎癥疾病和 COVID-19 的研究。
靶點

A3AR

體外研究

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.
體內(nèi)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.
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