| 貨號 | 規格 | 價格 | 上海 | 北京 | 武漢 | 南京 | 購買數量 |
|---|---|---|---|---|---|---|---|
S80417-2mg |
≥99% | ￥240.00 | 貨期：2-3天 | - | - | - |
|
S80417-5mg |
99.0% | ￥380.00 | 8 | - | - | - |
|
S80417-10mg |
99.0% | ￥490.00 | 5 | - | - | - |
|
S80417-25mg |
99.0% | ￥800.00 | 6 | - | - | - |
|
S80417-50mg |
99.0% | ￥1220.00 | 5 | - | - | - |
|
S80417-100mg |
≥99% | ￥2080.00 | 貨期：2-3天 | - | - | - |
|
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
| 產品描述： | 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 | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點： | IC50: 15 nM (A2A receptor);AdenosineReceptor | ||||||||||||||||||||
| 體外研究： | 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. | ||||||||||||||||||||
| 體內研究： | 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. | ||||||||||||||||||||
| 參考文獻： | 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 | ||||||||||||||||||||
| 保存條件： | -20℃ | ||||||||||||||||||||
| 配置溶液濃度參考： |
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| 注意： | 部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
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營業執照(三證合一)
北京