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Submit ReviewPSB 10 hydrochloride is a potent and highly selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1, A2A and A2B receptors (Ki values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A1 and A2A receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 4 nM). Produces thermal hyperalgesia in mice in vivo.
PSB 10 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 435.14 |
公式 | C16H14Cl3N5O.HCl |
储存 | Desiccate at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 591771-91-4 |
PubChem ID | 90488733 |
InChI Key | JUPMOTHIKGWECW-DDWIOCJRSA-N |
Smiles | CC[C@H](C3)N=C1N3C(N(C)C2=C1NC(C4=C(Cl)C(Cl)=CC(Cl)=C4)=N2)=O.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 10.88 | 25 | |
ethanol | 4.35 | 10 |
以下数据基于产品分子量 435.14。 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 |
---|---|---|---|
0.25 mM | 9.19 mL | 45.96 mL | 91.92 mL |
1.25 mM | 1.84 mL | 9.19 mL | 18.38 mL |
2.5 mM | 0.92 mL | 4.6 mL | 9.19 mL |
12.5 mM | 0.18 mL | 0.92 mL | 1.84 mL |
参考文献是支持产品生物活性的出版物。
Muller (2003) Medicinal chemistry of adenosine A3 receptor ligands. Curr.Top.Med.Chem. 3 445 PMID: 12570761
Ozola et al (2003) 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors. Bioorg.Med.Chem. 11 347 PMID: 12517430
Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358 PMID: 14563788
If you know of a relevant reference for PSB 10 hydrochloride, please let us know.
关键词: PSB 10 hydrochloride, PSB 10 hydrochloride supplier, Potent, selective, human, A3, receptors, antagonists, inverse, agonists, adenosines, PSB10, hydrochloride, HCl, Adenosine, Receptors, 2010, Tocris Bioscience
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