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Submit ReviewUCPH 101 is a selective non-substrate inhibitor of EAAT1 (IC50 values are 660, >300000 and >300000 nM for EAAT1, EAAT2 and EAAT3 respectively). Also demonstrates no significant inhibition at EAAT4 or EAAT5 in a patch-clamp electrophysiology assay (at final concentration up to 10 μM).
分子量 | 422.48 |
公式 | C27H22N2O3 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1118460-77-7 |
PubChem ID | 25223366 |
InChI Key | YBMGNDPBARCLFT-UHFFFAOYSA-N |
Smiles | NC2=C(C#N)C(C3=CC=C(OC)C=C3)C1=C(O2)CC(C4=C(C=CC=C5)C5=CC=C4)CC1=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 10.56 | 25 |
以下数据基于产品分子量 422.48。 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 | 9.47 mL | 47.34 mL | 94.68 mL |
1.25 mM | 1.89 mL | 9.47 mL | 18.94 mL |
2.5 mM | 0.95 mL | 4.73 mL | 9.47 mL |
12.5 mM | 0.19 mL | 0.95 mL | 1.89 mL |
参考文献是支持产品生物活性的出版物。
Jensen et al (2009) Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J.Med.Chem. 52 912 PMID: 19161278
Erichsen et al (2010) Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101). J.Med.Chem. 53 7180 PMID: 20857912
Bunch et al (2009) Excitatory amino acid transporters as potential drug targets. Exp.Opin.Ther.Targets 13 719
Abrahamsen et al (2013) Allosteric modulation of an excitatory amino acid transporter: The subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J.Neurosci. 33 1068 PMID: 23325245
If you know of a relevant reference for UCPH 101, please let us know.
关键词: UCPH 101, UCPH 101 supplier, Selective, non-substrate, EAAT1, inhibitors, inhibits, excitatory, amino, acid, transporters, glutamate, monoamine, neurotransmitter, GLAST, UCPH101, Glutamate, Transporters, 3490, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 UCPH 101 的部分引用包括:
Brancaccio et al (2017) Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling. Neuron 93 1420 PMID: 28285822
Liang et al (2014) δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes. Vision Res 171 5417 PMID: 25052197
Tse et al (2014) Pharmacological inhibitions of glutamate transporters EAAT1 and EAAT2 compromise glutamate transport in photoreceptor to ON-bipolar cell synapses. PLoS One 103 49 PMID: 25152321
Dumont et al (2014) Differential regulation of glutamate transporter subtypes by pro-inflammatory cytokine TNF-α in cortical astrocytes from a rat model of amyotrophic lateral sclerosis. Stroke 9 e97649 PMID: 24836816
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.