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TrkA-IN-23

Chemical Structure : TrkA-IN-23

CAS No.: 1821484-84-7

TrkA-IN-23 (TrkA inhibitor)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 524.402
    Formula C26H23Cl2N5O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

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

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