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Submit ReviewJNJ 47965567
说明： Potent and selective P2X7 antagonist; brain penetrant
化学名： 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for JNJ 47965567
JNJ 47965567 is a potent and selective P2X7 antagonist (pIC50 values are 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively). Selective over a panel of 50 other receptors, ion channels and transporters. Reduces BzATP-induced IL-1β release from monocytes in vitro and from rat brain in vivo. Attenuates amphetamine-induced hyperactivity in rats. Brain penetrant.
化合物库 for JNJ 47965567
JNJ 47965567 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 JNJ 47965567
| 分子量 | 488.64 |
| 公式 | C28H32N4O2S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1428327-31-4 |
| PubChem ID | 66553218 |
| InChI Key | XREFXUCWSYMIOG-UHFFFAOYSA-N |
| Smiles | O=C(NCC4(CCOCC4)N3CCN(C5=CC=CC=C5)CC3)C1=CC=CN=C1SC2=CC=CC=C2 |
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 JNJ 47965567
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| 1eq. HCl | 24.43 | 50 | |
| DMSO | 48.86 | 100 |
制备储备液 for JNJ 47965567
以下数据基于产品分子量 488.64。 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 |
|---|---|---|---|
| 1 mM | 2.05 mL | 10.23 mL | 20.46 mL |
| 5 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 10 mM | 0.2 mL | 1.02 mL | 2.05 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
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产品说明书 for JNJ 47965567
参考文献 for JNJ 47965567
参考文献是支持产品生物活性的出版物。
Bhattacharya et al (2013) Pharmacological characterization of a novel centrally permeable P2X7 receptor antagonist: JNJ-47965567. Br.J.Pharmacol. 170 624 PMID: 23889535
Letavic et al (2013) Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists. ACS Med.Chem.Lett. 12 419 PMID: 24900687
If you know of a relevant reference for JNJ 47965567, please let us know.
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关键词: JNJ 47965567, JNJ 47965567 supplier, JNJ47965567, potent, selective, p2x7, purinergics, antagonists, brain, penetrant, P2X, Receptors, 5299, Tocris Bioscience
4 篇 JNJ 47965567 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JNJ 47965567 的部分引用包括：
Uderhardt et al (2019) Resident Macrophages Cloak Tissue Microlesions to Prevent Neutrophil-Driven Inflammatory Damage. Cell 177 541 PMID: 30955887
Rita et al (2018) Microglial glutamate release evoked by α-synuclein aggregates is prevented by dopamine. Glia 66 2353-2365 PMID: 30394585
Andras et al (2022) Detection and Functional Evaluation of the P2X7 Receptor in hiPSC Derived Neurons and Microglia-Like Cells. Front Mol Neurosci 14 793769 PMID: 35095416
McEwan et al (2021) Autocrine regulation of wound healing by ATP release and P2Y 2 receptor activation Life Sci 283 119850 PMID: 34314735
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JNJ 47965567 的评论
平均评分: 4.3 (基于 3 条评论。)
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Good inhibitor.
By
Stefan Uderhardt on 06/06/2020
分析类型： In Vivo
种属： Mouse
细胞系/组织： phagocyte
DMSO dilution 100 μM
In vivo usage.
By
Spandita Dutta on 08/07/2018
分析类型： In Vivo
种属： Mouse
细胞系/组织： Hippocampal neurons
I have used this product emulsified in 30% sulphoxymethylester, and injected them sub-cutaneously to study IL-1beta release mechanism in the hippocampus of the brain. I am currently working on its effect on hippocampal neurons in culture.
Followed publication by Bhattacharya et al, Br J Pharmacol. 2013 Oct;170(3):624-40. doi: 10.1111/bph.12314 for in vivo and in vitro usage.
P2X7 blocker.
By
Anonymous on 01/31/2018
分析类型： Ex Vivo
种属： Mouse
Used to block a potentially P2X7-dependent process, but no effect was observed. No positive control so unsure if the drug actually blocked its target. More experiments needed.
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.