IB-MECA (IB-MECA) 是一流的、具有口服活性和选择性的 A3 腺苷受体 (A3AR) 激动剂。
Cas No. | 152918-18-8 |
别名 | IB-MECA; CF-101 |
Canonical SMILES | O[C@H]1[C@H](N2C=NC3=C(NCC4=CC=CC(I)=C4)N=CN=C23)O[C@H](C(NC)=O)[C@H]1O |
分子式 | C18H19IN6O4 |
分子量 | 510.29 |
溶解度 | DMSO : ≥ 45 mg/mL (88.19 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | IB-MECA is an agonist of the adenosine A3 receptor with EC50 values of 0.11 uM. IC50 value: 0.11 uM (EC50) [3]Target: adenosine A3 receptorin vitro: IB-MECA has been shown to play important roles in cell proliferation and apoptosis in a variety of cancer cell lines. TheIB-MECA was capable of decreasing intracellular cyclic adenosine monophosphate (cAMP) that was the reason for the presence of functional A3 adenosine receptor on the cell lines. IB-MECA significantly reduced cell viability in a dose-dependent manner. IB-MECA, an A3AR agonist, inhibits the growth of different cancer cell types like melanoma, colon, breast, leukemia, and prostateIB-MECA was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 0.82 uM in OVCAR-3 cells. IB-MECA was able to inhibit forskolin-stimulated cAMP levels with an EC50 value of 1.2 uM in Caov-4 cells.in vivo: Administrations of single intraperitoneal doses of either IB-MECA 0.5 h post-irradiation resulted in statistically significant increases of MST in comparison with the control irradiated mice.[2] References: [1]. Hofer M, et al. Agonist of the adenosine A3 receptor, IB-MECA, and inhibitor of cyclooxygenase-2, meloxicam, given alone or in a combination early after total body irradiation enhance survival of γ-irradiated mice. Radiat Environ Biophys. 2014 Mar;53(1):2 [2]. Abedi H, et al. Mitochondrial and caspase pathways are involved in the induction of apoptosis by IB-MECA in ovarian cancer cell lines. Tumour Biol. 2014 Nov;35(11):11027-11039. [3]. Shin Y, et al. Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors Drug Dev Res. 1996 Sep 1;39(1):36-46. |