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MRS 1220

Cat. No. 1217 13 篇引用文献 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Highly potent and selective hA3 antagonist
化学名： N-[9-Chloro-2-(2-furanyl)[1,2,4]-triazolo[1,5-c]quinazolin-5-yl]benzene acetamide
纯度： ≥98% (HPLC)
说明书
引用文献 (13)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for MRS 1220

MRS 1220 is a potent and highly selective antagonist at the human A3 adenosine receptor (Ki values are 0.65, 305, and 52 nM at hA3, rA1 and rA2A respectively. Displays an IC50 value > 1 μM for inhibition of binding to rat A3 receptors).

许可信息

Sold with the permission of the NIH, US Patent 60/029,855

化合物库 for MRS 1220

MRS 1220 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for MRS 1220

分子量 403.83
公式 C21H14ClN5O2
储存 Store at RT
纯度 ≥98% (HPLC)
CAS Number 183721-15-5
PubChem ID 393595
InChI Key TWWFAXQOKNBUCR-UHFFFAOYSA-N
Smiles ClC1=CC=C2N=C(NC(=O)CC3=CC=CC=C3)N3N=C(N=C3C2=C1)C1=CC=CO1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for MRS 1220

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 8.08 20 温和加热

制备储备液 for MRS 1220

以下数据基于产品分子量 403.83。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 12.38 mL 61.91 mL 123.81 mL
1 mM 2.48 mL 12.38 mL 24.76 mL
2 mM 1.24 mL 6.19 mL 12.38 mL
10 mM 0.25 mL 1.24 mL 2.48 mL

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产品说明书 for MRS 1220

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for MRS 1220

参考文献是支持产品生物活性的出版物。

Jacobson et al (1997) Pharmacological characterization of novel A3 adenosine receptor selective antagonists. Neuropharmacology 36 1157 PMID: 9364471

Kim et al (1996) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) are selective for the human A3 receptor subtype. J.Med.Chem. 39 4142 PMID: 8863790

Kim et al (1998) Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. J.Med.Chem. 41 2835 PMID: 9667972

If you know of a relevant reference for MRS 1220, please let us know.

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关键词: MRS 1220, MRS 1220 supplier, potent, selective, hA3, antagonists, Receptors, adenosines, MRS1220, Adenosine, A3, 1217, Tocris Bioscience

13 篇 MRS 1220 的引用文献

引用文献是使用了 Tocris 产品的出版物。 MRS 1220 的部分引用包括：

Torres et al (2016) Adenosine A3 receptor elicits chemoresistance mediated by multiple resistance-associated protein-1 in human glioblastoma stem-like cells. Oncotarget 7 67373 PMID: 27634913

Stoddart et al (2012) Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay. Chem Biol 19 1105 PMID: 22999879

Long et al (2010) Adenosine receptor regulation of coronary blood flow in Ossabaw miniature swine. Am J Physiol Gastrointest Liver Physiol 335 781 PMID: 20855445

Kinoshita et al (2018) Anti-Depressant Flu Reveals its Therapeutic Effect Via Astrocytes. EBioMedicine 32 72 PMID: 29887330

Liu et al (2018) Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect. Brain Res 1700 47 PMID: 29935155

Stoddart et al (2015) Application of BRET to monitor ligand binding to GPCRs. Nat Methods 12 661 PMID: 26030448

Corriden et al (2014) Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. FASEB J 28 4211 PMID: 24970394

Liñán-Rico et al (2015) Neuropharmacology of purinergic receptors in human submucous plexus: Involvement of P2X?, P2X?, P2X? channels, P2Y and A? metabotropic receptors in neurotransmission. Neuropharmacology 95 83 PMID: 25724083

Kozma et al (2013) Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor. Biochem Pharmacol 85 1171 PMID: 23376019

Germack and Dickenson (2004) Characterization of ERK1/2 signalling pathways induced by adenosine receptor subtypes in newborn rat cardiomyocytes. Br J Pharmacol 141 329 PMID: 14751870

Man et al (2003) Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. Br J Pharmacol 139 172 PMID: 12746236

Wen and Knowles (2003) Extracellular ATP and adenosine induce cell apoptosis of human hepatoma Li-7A cells via the A3 adenosine receptor. Br J Pharmacol 140 1009 PMID: 14530217

Pugliese et al (2006) A3 adenosine receptor antagonists delay irreversible synaptic failure caused by oxygen and glucose deprivation in the rat CA1 hippocampus in vitro. Br J Pharmacol 147 524 PMID: 16415905

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