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Chemical Structure : TrkA-IN-23
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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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.
| M.Wt | 524.402 | |
| Formula | C26H23Cl2N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Bagal SK, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.8b00280.
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