SCH-58261 - Adenosine Receptor Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESCH 58261Cat. No.: HY-19533CAS No.: 160098-96-4分式: CHNO分量: 345.36作靶点: Adenosine Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 34 mg/mL (98.45 mM)* means soluble

2、, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8955 mL 14.4776 mL 28.9553 mL5 mM 0.5791 mL 2.8955 mL 5.7911 mL10 mM 0.2896 mL 1.4478 mL 2.8955 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 SCH 58261种强效、选择性的竞争性腺苷 A2A 受体拮抗剂，IC50 值为 15 nM，对 A2A 受体的选

3、择性分别是A1、A2B 和 A3 受体的 323 倍、53 倍、100 倍 1 2 3。IC50 & Target IC50: 15 nM (A2A receptor) 2体外研究SCH 58261 (0 nM10 M; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEline H1975 4.SCH58261 (25 M; 72 hours) can inhibit the growth

4、 of CAF cells 5.Cell Viability Assay 4Cell Line: H1975 cellsConcentration: 10 nM-10 MIncubation Time: 7 daysResult: Produced a concentration-dependent decrease in H1975 cell growth.Cell Proliferation Assay 5Cell Line: CAF cellsConcentration: 25 MIncubation Time: 72 hoursResult: Inhibit the growth of

5、 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 mousemodel 5.SCH 58261 (5 mg/kg; i.p.; 3 times; every 3 hours; 10 minutes before haloperidol) partially decreases thehaloperidol-induced catalepsy and the increase in the PENK mRN

6、A expression in both dorsolateral andventrolateral parts of the striatum at all three examined levels 6.SCH 58261 diminishes the parkinsonian-like muscle rigidity and potentiates the effect of L-DOPA in ratmodel 7.Animal Model: 46 weeks old athymic nude mice (NCI) with PC9 cells xenograft 5Dosage: 2

7、 mg/kgAdministration: Intraperitoneal injection; daily; for 20 daysResult: Decreased tumor growth.户使本产品发表的科研献 Cell Signal. 2019 Mar 7;58:44-52.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Zocchi C, et al. Binding of the radiol

8、igand 3H-SCH 58261, a new non-xanthine A2A adenosine receptor antagonist, to rat striatalmembranes. 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 by3H-CGS 21680 binding. Br J

9、 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 MolCell Cardiol. 2009 Nov;47(5):684-90.4. Kuzumaki N, et al. Multiple analyses of G-protein coupled receptor (GPCR) expressio

10、n in the development of gefitinib-resistance intransforming 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 cancerassociated fibroblasts inhibits their growth. Cancer Biol The

11、r. 2013 Sep;14(9):860-8.6. Wardas J, et al. SCH 58261, a selective adenosine A2A receptor antagonist, decreases the haloperidol-enhanced proenkephalin mRNAexpression 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.McePdfHeightCaution: Product has