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说明： Potent group I mGlu antagonist
化学名： N-Phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide
纯度： ≥98% (HPLC)
生物活性 for PHCCC
PHCCC is a group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM); 67 times more potent than (S)-4-carboxyphenylglycine (Cat. No. 0323). Also a positive allosteric modulator for mGlu4a; potentiates L-AP4-mediated inhibition of striatopallidal synaptic transmission in vitro. Displays antiParkinsonian effects in rats in vivo.
许可信息
Sold for research purposes under license from Suntory Ltd.
化合物库 for PHCCC
PHCCC 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 PHCCC
| 分子量 | 294.31 |
| 公式 | C17H14N2O3 |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 179068-02-1 |
| PubChem ID | 5866327 |
| InChI Key | FPXPIEZPAXSELW-CYVLTUHYSA-N |
| Smiles | O=C(NC4=CC=CC=C4)C3(C2C3)OC1=CC=CC=C1/C2=N/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 PHCCC
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 29.43 | 100 |
制备储备液 for PHCCC
以下数据基于产品分子量 294.31。 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 | 3.4 mL | 16.99 mL | 33.98 mL |
| 5 mM | 0.68 mL | 3.4 mL | 6.8 mL |
| 10 mM | 0.34 mL | 1.7 mL | 3.4 mL |
| 50 mM | 0.07 mL | 0.34 mL | 0.68 mL |
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产品说明书 for PHCCC
参考文献 for PHCCC
参考文献是支持产品生物活性的出版物。
Mao and Wang (2001) Selective activation of group I metabotropic glutamate receptors upregulates preprodynorphin, substance P and preproenkephalin mRNA expression in rat dorsal striatum. Synapse 39 82 PMID: 11071713
Marino et al (2003) Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc.Natl.Acad.Sci.USA 100 13668 PMID: 14593202
Annoura et al (1996) A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates. Bioorg.Med.Chem.Lett. 6 763
Flor et al (2002) Positive allosteric modulators of metabotropic glutamate receptor subtype 4: pharmacological and molecular characterization. Neuropharmacology 43 286 Abstr.No. 47
If you know of a relevant reference for PHCCC, please let us know.
关键词: PHCCC, PHCCC supplier, Potent, group, I, mGlur, antagonists, Group, Receptors, mGlu1, mGlu5, Glutamate, Metabotropic, mGlu4, (Metabotropic), 1027, Tocris Bioscience
8 篇 PHCCC 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PHCCC 的部分引用包括：
Spampinato et al (2015) Glial metabotropic glutamate receptor-4 increases maturation and survival of oligodendrocytes. Biol Psychiatry 8 462 PMID: 25642169
Volpi et al (2016) Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells. Neuropharmacology 102 59 PMID: 26522434
Broadstock et al (2012) Antiparkinsonian potential of targeting group III metabotropic glutamate receptor subtypes in the rodent substantia nigra pars reticulata. Br J Pharmacol 165 1034 PMID: 21627638
Niswender et al (2008) Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol 74 1345 PMID: 18664603
Jones et al (2011) Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 ( J Med Chem 54 7639 PMID: 21966889
Foong (2009) mGluR(1) Receptors Contribute to Non-Purinergic Slow Excitatory Transmission to Submucosal VIP Neurons of Guinea-Pig Ileum. Front Neurosci 3 46 PMID: 20582273
Hemstapat et al (2006) A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol 70 616 PMID: 16645124
Collard et al (2002) Neutrophil-derived glutamate regulates vascular endothelial barrier function. J Biol Chem 277 14801 PMID: 11847215
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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。
Metabotropic Glutamate Receptors Scientific Review
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