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Submit ReviewAZ 11645373
说明： Potent and selective human P2X7 antagonist
化学名： 3-[1-[[(3'-Nitro[1,1'-biphenyl]-4-yl)oxy]methyl]-3-(4-pyridinyl)propyl]-2,4-thiazolidinedione
纯度： ≥98% (HPLC)
生物活性 for AZ 11645373
AZ 11645373 is a potent and selective human P2X7 antagonist (KB values are 5 - 7 and > 10,000 nM at hP2X7 and rP2X7 respectively) that is completely without effect at all other P2X subtypes. Inhibits BzATP-mediated calcium influx and inhibits ATP-mediated IL-1β release in vitro (KB values are 15 and 92 nM respectively).
许可信息
Sold for research purposes under agreement from AstraZeneca
技术数据 for AZ 11645373
| 分子量 | 463.51 |
| 公式 | C24H21N3O5S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 227088-94-0 |
| PubChem ID | 9804433 |
| InChI Key | VQEHBLGYANQWEA-UHFFFAOYSA-N |
| Smiles | O=C(CSC4=O)N4C(COC2=CC=C(C3=CC=CC([N+]([O-])=O)=C3)C=C2)CCC1=CC=NC=C1 |
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 AZ 11645373
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 4.64 | 10 |
制备储备液 for AZ 11645373
以下数据基于产品分子量 463.51。 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 |
|---|---|---|---|
| 0.1 mM | 21.57 mL | 107.87 mL | 215.75 mL |
| 0.5 mM | 4.31 mL | 21.57 mL | 43.15 mL |
| 1 mM | 2.16 mL | 10.79 mL | 21.57 mL |
| 5 mM | 0.43 mL | 2.16 mL | 4.31 mL |
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产品说明书 for AZ 11645373
参考文献 for AZ 11645373
参考文献是支持产品生物活性的出版物。
Stokes et al (2006) Characterization of a selective and potent antagonist of human P2X7 receptors, AZ11645373. Br.J.Pharmacol. 149 880 PMID: 17031385
Michel et al (2009) Mechanism of action of species-selective P2X(7) receptor antagonists. Br.J.Pharmacol. 156 1312 PMID: 19309360
Alcaraz et al (2003) Novel P2X7 receptor antagonists. Bioorg.Med.Chem.Letts. 13 4043
If you know of a relevant reference for AZ 11645373, please let us know.
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关键词: AZ 11645373, AZ 11645373 supplier, Potent, selective, human, P2X7, antagonists, Receptors, Purinergic, purinoceptors, AZ11645373, AstraZeneca, P2X, 3317, Tocris Bioscience
7 篇 AZ 11645373 的引用文献
引用文献是使用了 Tocris 产品的出版物。 AZ 11645373 的部分引用包括：
Sathanoori et al (2015) The ATP Receptors P2X7 and P2X4 Modulate High Glucose and Palmitate-Induced Inflammatory Responses in Endothelial Cells. PLoS One 10 e0125111 PMID: 25938443
Kawano et al (2015) Autocrine Regulation of UVA-Induced IL-6 Production via Release of ATP and Activation of P2Y Receptors. PLoS One 10 e0127919 PMID: 26030257
Foster et al (2013) Mitochondrial superoxide generation enhances P2X7R-mediated loss of cell surface CD62L on naive human CD4+ T lymphocytes. J Immunol 190 1551 PMID: 23319734
Agrawal et al (2016) P2X7Rs are involved in cell death, growth and cellular signaling in primary human osteoblasts Bone 95 91 PMID: 27856358
Bhaskaracharya et al (2014) Probenecid blocks human P2X7 receptor-induced dye uptake via a pannexin-1 independent mechanism. PLoS One 9 e93058 PMID: 24671093
Soares-Bezerra et al (2015) An Improved Method for P2X7R Antagonist Screening. Arthritis Rheumatol 10 e0123089 PMID: 25993132
Karmakar et al (2016) Neutrophil P2X7 receptors mediate NLRP3 inflammasome-dependent IL-1β secretion in response to ATP. Nat.Commun. 7 10555 PMID: 26877061
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
P2X and P2Y Receptors Scientific Review
Written by Kenneth Jacobson, this review provides an overview of the different subtypes and structures of the P2 receptor families, as well as the pharmacological probes used to study them; compounds available from Tocris are listed.