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Submit ReviewGS 6201
说明： Selective A2B antagonist
别名： CVT 6883
化学名： 3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione
纯度： ≥99% (HPLC)
生物活性 for GS 6201
GS 6201 is a selective antagonist of adenosine A2B receptors (Ki values are 22, 1070, 1940 and 3280 nM for human A2B, A3, A1 and A2A receptors respectively). Attenuates allergen-, NECA- and AMP-induced airway reactivity in an allergic mouse model of asthma. Also shown to attenuate the inflammatory response during acute myocardial infarction in mice; reduces caspase-1 activity in the heart.
化合物库 for GS 6201
GS 6201 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 GS 6201
| 分子量 | 446.43 |
| 公式 | C21H21F3N6O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 752222-83-6 |
| PubChem ID | 11270783 |
| InChI Key | KOYXXLLNCXWUNF-UHFFFAOYSA-N |
| Smiles | O=C(N(CC)C2=C1NC(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)=N2)N(CCC)C1=O |
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 GS 6201
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 2.23 | 5 |
制备储备液 for GS 6201
以下数据基于产品分子量 446.43。 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.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.05 mM | 44.8 mL | 224 mL | 448 mL |
| 0.25 mM | 8.96 mL | 44.8 mL | 89.6 mL |
| 0.5 mM | 4.48 mL | 22.4 mL | 44.8 mL |
| 2.5 mM | 0.9 mL | 4.48 mL | 8.96 mL |
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产品说明书 for GS 6201
参考文献 for GS 6201
参考文献是支持产品生物活性的出版物。
Elzein et al (2008) Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J.Med.Chem. 51 2267 PMID: 18321039
Toldo et al (2012) GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J.Pharmacol.Exp.Ther. 343 587 PMID: 22923737
Mustafa et al (2007) Effect of a specific and selective A2B adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. J.Pharmacol.Exp.Ther. 320 1246 PMID: 17159162
If you know of a relevant reference for GS 6201, please let us know.
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关键词: GS 6201, GS 6201 supplier, GS6201, CVT6883, asthma, adenosine, A2B, antagonists, allergy, antiallergics, selective, CVT, 6883, Adenosine, Receptors, 4727, Tocris Bioscience
3 篇 GS 6201 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GS 6201 的部分引用包括：
Qun et al (2019) The Role of Adenosine A2b Receptor in Mediating the Cardioprotection of Electroacupuncture Pretreatment via Influencing Ca2+ Key Regulators. Evid Based Complement Alternat Med 2019 6721286 PMID: 31885657
Mertens et al (2018) Switching-Off Adora2b in Vascular Smooth Muscle Cells Halts the Development of Pulmonary Hypertension. Front Physiol 9 555 PMID: 29910735
Perez-Aso et al (2015) A novel phosphodiesterase 4 (PDE4) inhibitor, regulates inflammation through multiple cAMP downstream effectors. Arthritis Res Ther 17 249 PMID: 26370839
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