製品の概要

  • 製品名
    UCPH-102, EAAT1 inhibitor
  • 製品の詳細
    Selective EAAT1 inhibitor
  • 生理活性の詳細
    Selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor (IC50 = 0.42 μM). Active in vivo. Blood-brain barrier permeable analog of UCPH-101 (ab120309).
  • 精製度
    > 98%
  • CAS 番号
    1229591-56-3
  • 構造式
    Chemical Structure

製品の特性

  • 体系名
    2-Amino-5,6,7,8-tetrahydro-4-methyl-7-(1-naphthalenyl)-5-oxo-4H-1-benzopyran-3-carbonitrile
  • 分子量
    330.39
  • 分子式
    C21H18N2O2
  • 保存方法
    Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
  • 溶解性
    Soluble in DMSO to 25 mM. It is recommended that all preparations are centrifuged before use.
  • 使用に関する注意

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES 線形表記
    O=C1CC(CC=2OC(N)=C(C#N)C(C)C1=2)c4cccc3ccccc34
  • 由来

    Synthetic

画像

  • Plot to compare the bioavailability of UCPH-102 in plasma versus brain.

参考文献

This product has been referenced in:
  • Erichsen MN  et al. Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs. Neurochem Res 39:1964-79 (2014). Read more (PubMed: 24682739) »
  • Abrahamsen B  et al. 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 33:1068-87 (2013). Read more (PubMed: 23325245) »
  • Huynh TH  et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem 20:6831-9 (2012). Read more (PubMed: 23072958) »

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