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SCH58261 {[allProObj[0].p_purity_real_show]}

货号:A144938

SCH58261是一个强效且选择性的A2a腺苷受体拮抗剂,其Ki值分别为2.3 nM(rat A2a)和2 nM(bovine A2a)。

SCH58261 化学结构 CAS号:160098-96-4
SCH58261 化学结构
CAS号:160098-96-4
SCH58261 3D分子结构
CAS号:160098-96-4
SCH58261 化学结构 CAS号:160098-96-4
SCH58261 3D分子结构 CAS号:160098-96-4
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SCH58261 纯度/质量文件 产品仅供科研

货号:A144938 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adenosine Receptor 其他靶点 纯度
ZM241385 99%+
Istradefylline +++

Adenosine A2A receptor, Ki: 2.2 nM

98%
Reversine +

human A3 adenosine receptor, Ki: 0.66 μM

98%
SCH58261 ++++

bovine A2a, Ki: 2.0 nM

rat A2a, Ki: 2.3 nM

99%+
A2A receptor antagonist 1 ++

A1R, Ki: 264 nM

A2AR, Ki: 4 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

SCH58261 生物活性

靶点
  • Adenosine Receptor

    bovine A2a, Ki:2.0 nM

    rat A2a, Ki:2.3 nM

描述 Adenosine modulates a variety of physiological functions acting via specific cell surface receptors which are divided into at least four subtypes: A1, A2a, A2b and A3. The A2a receptor subtype which is coupled to stimulation of adenylyl cyclase, is a high affinity receptor found in large amounts in the brain striatum. In the periphery, the A2a receptor is localized in different organs and tissues, including platelets, neutrophils and vascular smooth muscle cells [10]. SCH 58261 is an efficient and selective A2a adenosine receptor antagonist, with Ki values of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively, and displays 50- to 100-fold more selective for A2a receptor than A1, and shows no affinity for either the A3 adenosine receptor or other receptors at concentrations up to 1 mM in rat and bovine brain, respectively [11]. SCH 58261 (0 nM–10 µM; 7 days) decreases cell viability in a concentration-dependent in the NSCLC cell line H1975 [12]. It also antagonized competitively the effects induced by the A2a adenosine-selective agonist CGS 21680 in two functional assays, such as inhibition of rabbit platelet aggregation and porcine coronary artery relaxation [13]. SCH58261, systemically administered (0.01 mg/kg intraperitoneal. 1, 6 and 10 hours after spinal cord injury (SCI)), reduced demyelination and levels of TNF-α, Fas-L, PAR, Bax expression and activation of JNK mitogen-activated protein kinase (MAPK) 24 hours after SCI [14]. 6-OHDA (8 μg/rat, Intra-SNc) induced motor disorders of Parkinson's disease and increased elapsed time in the beam test (p<0.001). Injection of SCH-58261 (2 mg/kg, i.p.) attenuated elapsed time on beam (p<0.01 and p<0.001), which indicated administration of SCH-58261 can improve the 6-OHDA-induced bradykinesia and motor disturbance [15].

SCH58261 动物研究

Dose Mice: 0.1 mg/kg - 1 mg/kg[3] (i.p.), 2 mg/kg[4] (i.p.), 1 mg/kg - 10 mg/kg[5] (i.p.) Rat: 0.01 mg/kg - 1 mg/kg[6] (i.p.), 5 mg/kg[7] (i.p.); 0.5 mg/kg[8] (p.o.)
Administration i.p., p.o.
Pharmacokinetics
Animal Rats[9]
Dose 0.5 mg/kg
Administration i.v.
Cmax 109 ng/ml
T1/2 26.7 min
F 0.757

SCH58261 参考文献

[1]Paterniti I, Melani A, et al. Selective adenosine A2A receptor agonists and antagonists protect against spinal cord injury through peripheral and central effects. J Neuroinflammation. 2011 Apr 12;8:31.

[2]Zocchi C, Ongini E, et al. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[3]Pagnussat N, Almeida AS, et al. Adenosine A(2A) receptors are necessary and sufficient to trigger memory impairment in adult mice. Br J Pharmacol. 2015 Aug;172(15):3831-45.

[4]Hsu CW, Wang CS, et al. Caffeine and a selective adenosine A2A receptor antagonist induce sensitization and cross-sensitization behavior associated with increased striatal dopamine in mice. J Biomed Sci. 2010 Jan 15;17:4.

[5]El Yacoubi M, Ledent C, et al. SCH 58261 and ZM 241385 differentially prevent the motor effects of CGS 21680 in mice: evidence for a functional 'atypical' adenosine A(2A) receptor. Eur J Pharmacol. 2000 Jul 28;401(1):63-77.

[6]Popoli P, Pintor A, et al. Blockade of striatal adenosine A2A receptor reduces, through a presynaptic mechanism, quinolinic acid-induced excitotoxicity: possible relevance to neuroprotective interventions in neurodegenerative diseases of the striatum. J Neurosci. 2002 Mar 1;22(5):1967-75.

[7]Wardas J, Pietraszek M, 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.

[8]Leite MR, Wilhelm EA, et al. Protective effect of caffeine and a selective A2A receptor antagonist on impairment of memory and oxidative stress of aged rats. Exp Gerontol. 2011 Apr;46(4):309-15.

[9]Yang M, Soohoo D, et al. Characterization of the potency, selectivity, and pharmacokinetic profile for six adenosine A2A receptor antagonists. Naunyn Schmiedebergs Arch Pharmacol. 2007 Apr;375(2):133-44. Epub 2007 Feb 20.

[10]Varani K. 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.

[11]Zocchi C. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[12]Kuzumaki N. 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. doi: 10.1371/journal.pone.0044368.

[13] Zocchi C. The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. J Pharmacol Exp Ther. 1996 Feb;276(2):398-404.

[14]Paterniti I. Selective adenosine A2A receptor agonists and antagonists protect against spinal cord injury through peripheral and central effects. J Neuroinflammation. 2011 Apr 12;8:31. doi: 10.1186/1742-2094-8-31.

[15]Reyhani-Rad S, Mahmoudi J. Effect of adenosine A2A receptor antagonists on motor disorders induced by 6-hydroxydopamine in rat. Acta Cir Bras. 2016 Feb;31(2):133-7.

SCH58261 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.90mL

0.58mL

0.29mL

14.48mL

2.90mL

1.45mL

28.96mL

5.79mL

2.90mL

SCH58261 技术信息

CAS号160098-96-4
分子式C18H15N7O
分子量 345.358
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Inert atmosphere,2-8°C

溶解方案

DMSO: 35 mg/mL(101.34 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

4% DMSO40% PEG 300+4% Tween 80++water 2 mg/mL

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