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Submit ReviewPNU 120596
说明： Positive allosteric modulator of α7 nAChRs; active in vivo
化学名： N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea
纯度： ≥99% (HPLC)
生物活性 for PNU 120596
PNU 120596 is a positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.
化合物库 for PNU 120596
PNU 120596 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 PNU 120596
| 分子量 | 311.72 |
| 公式 | C13H14ClN3O4 |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 501925-31-1 |
| PubChem ID | 311434 |
| InChI Key | CEIIEALEIHQDBX-UHFFFAOYSA-N |
| Smiles | COC1=CC(OC)=C(Cl)C=C1NC(=O)NC1=NOC(C)=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 PNU 120596
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.17 | 100 |
制备储备液 for PNU 120596
以下数据基于产品分子量 311.72。 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 | 3.21 mL | 16.04 mL | 32.08 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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产品说明书 for PNU 120596
参考文献 for PNU 120596
参考文献是支持产品生物活性的出版物。
Hurst et al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066
Timmermann et al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074
Kalappa et al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819
If you know of a relevant reference for PNU 120596, please let us know.
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关键词: PNU 120596, PNU 120596 supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, active, vivo, Nicotinic, Receptors, Acetylcholine, PNU120596, PAM, (a7), 2498, Tocris Bioscience
15 篇 PNU 120596 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PNU 120596 的部分引用包括：
Kasheverov et al (2015) 6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor. Mar Drugs 13 1255 PMID: 25775422
Thomsen et al (2015) α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties. PLoS One 10 e0130572 PMID: 26086615
Noviello et al (2021) Structure and gating mechanism of the α7 nicotinic acetylcholine receptor. Cell 184 2121 PMID: 33735609
Barykin et al (2019) Isomerization of Asp7 in Beta-Amyloid Enhances Inhibition of the α7 Nicotinic Receptor and Promotes Neurotoxicity. Cells 8 PMID: 31349637
Pérez-Alvarez et al (2012) Pharmacological characterization of native α7 nicotinic ACh receptors and their contribution to depolarization-elicited exocytosis in human chromaffin cells. Br J Pharmacol 165 908 PMID: 21790533
Pandya and Yakel (2013) Activation of the α7 nicotinic ACh receptor induces anxiogenic effects in rats which is blocked by a 5-HT?a receptor antagonist. Neuropharmacology 70 35 PMID: 23321689
David et al (2010) Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes. Eur J Neurosci 31 978 PMID: 20377613
Bali et al (2019) Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo. Sci Rep 9 9324 PMID: 31249369
Gimenz-Gomez et al (2018) Increasing kynurenine brain levels reduces ethanol consumption in mice by inhibiting dopamine release in nucleus accumbens. Neuropharmacology 135 581 PMID: 29705534
Yamauchi et al (2012) Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. Nat Commun 82 687 PMID: 22784805
John et al (2015) Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. PLoS One 1601 15 PMID: 25553616
Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. PLoS One 10 e0125116 PMID: 25906356
Zhang et al (2015) Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor. Mol Pharmacol 10 e0137588 PMID: 26340537
daCosta et al (2015) Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors. J Neurosci 6 8057 PMID: 26282895
Maldifassi et al (2014) A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages. PLoS One 9 e108397 PMID: 25259522
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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。
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