| 产品描述： | SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively |
| 靶点： |
IC50: 15 nM (A2A receptor);AdenosineReceptor |
| 体外研究： |
SCH 58261 (0 nM–10 µM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975. SCH58261 (25 μM; 72 hours) can inhibit the growth of CAF cells. Cell Viability Assay Cell Line: H1975 cells Concentration: 10 nM-10 µM Incubation Time: 7 days Result: Produced a concentration-dependent decrease in H1975 cell growth. Cell Proliferation Assay Cell Line: CAF cells Concentration: 25 μM Incubation Time: 72 hours Result: Inhibit the growth of CAF1 and CAF2 cells. |
| 体内研究： |
SCH 58261 (2 mg/kg; i.p.; daily; for 20 days) causes a decrease in the tumor burden in a NSCLC mouse model. SCH 58261 (5 mg/kg; i.p.; 3 times; every 3 hours; 10 minutes before haloperidol) partially decreases the haloperidol-induced catalepsy and the increase in the PENK mRNA expression in both dorsolateral and ventrolateral parts of the striatum at all three examined levels. SCH 58261 diminishes the parkinsonian-like muscle rigidity and potentiates the effect of L-DOPA in rat model. Animal Model: 4‒6 weeks old athymic nude mice (NCI) with PC9 cells xenograft Dosage: 2 mg/kg Administration: Intraperitoneal injection; daily; for 20 days Result: Decreased tumor growth. |
| 参考文献： |
1. Zocchi C, et al. Binding of the radioligand [3H]-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatal membranes. Br J Pharmacol. 1996 Apr;117(7):1381-6. 2. Varani K, et al. Pharmacological and biochemical characterization of purified A2a adenosine receptors in human platelet membranes by [3H]-CGS 21680 binding. Br J Pharmacol. 1996 Apr;117(8):1693-701. 3. Xi J, et al. Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol. 2009 Nov;47(5):684-90. 4. Kuzumaki N, et al. Multiple analyses of G-protein coupled receptor (GPCR) expression in the development of gefitinib-resistance in transforming non-small-cell lung cancer. PLoS One. 2012;7(10):e44368. 5. Mediavilla-Varela M, et al. Antagonism of adenosine A2A receptor expressed by lung adenocarcinoma tumor cells and cancer associated fibroblasts inhibits their growth. Cancer Biol Ther. 2013 Sep;14(9):860-8. 6. Wardas J, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNA expression in the rat striatum. Brain Res. 2003 Jul 11;977(2):270-7. 7. Wardas J, et al. SCH 58261, an A(2A) adenosine receptor antagonist, counteracts parkinsonian-like muscle rigidity in rats. Synapse. 2001 Aug;41(2):160-71. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.896 ml |
14.478 ml |
28.955 ml |
| 5 mM |
0.579 ml |
2.896 ml |
5.791 ml |
| 10 mM |
0.29 ml |
1.448 ml |
2.896 ml |
| 50 mM |
0.058 ml |
0.29 ml |
0.579 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京