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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Trk Receptor-TrkA-IN-23
TrkA-IN-23

Chemical Structure : TrkA-IN-23

CAS No.: 1821484-84-7

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TrkA-IN-23 (TrkA inhibitor)

货号: PC-63490Not For Human Use, Lab Use Only.

TrkA-IN-23 is a highly potent, subtype selective, peripherally restricted, allosteric TrkA inhibitor with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    TrkA-IN-23 is a highly potent, subtype selective, peripherally restricted, allosteric TrkA inhibitor with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays.
    TrkA-IN-23 exhibits exquisite TrkA selectivity with >95% inhibition of TrkA and <15% inhibition in 392 biochemical kinase assays.
    TrkA-IN-23 also exhibits 18-fold selectivity for the non-activated TrkA construct (TrkA non-activated enzyme IC50=4nM, TrkA activated enzyme IC50=74 nM); inhibits NGF induced phosphorylated ERK formation in native adult rat DRGs with IC50 of 57 nM.
    TrkA-IN-23 abolishes sensitization to capsaicin administration to NGFsensitised skin in vivo in anaesthetised rats.
    TrkA-IN-23 demonstrates efefctivity in UVIH model of inflammatory pain in rats.

    物理化学性质&存储条件

    分子量 524.402
    分子式 C26H23Cl2N5O3
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    5-(2,4-dichloro-5-(pyridin-2-yl)benzamido)-N-(2-hydroxy-2-methylpropyl)-1-phenyl-1Hpyrazole-3-carboxamide

    参考文献

    1. Bagal SK, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.8b00280.

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