TrkA inhibitor compound 23(TrkA-IN-23)
Names
[ CAS No. ]:
1821484-84-7
[ Name ]:
TrkA inhibitor compound 23(TrkA-IN-23)
Biological Activity
[Description]:
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; exhibits exquisite TrkA selectivity with >95% inhibition of TrkA and <15% inhibition in 392 biochemical kinase assays; 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, abolishes sensitization to capsaicin administration to NGFsensitised skin in vivo in anaesthetised rats; demonstrates efefctivity in UVIH model of inflammatory pain in rats.
[References]
References 1. Bagal SK, et al. J Med Chem. 2018 May 3. doi: 10.1021/acs.jmedchem.8b00280. View Related Products by Target Trk Receptor
Chemical & Physical Properties
[ Molecular Formula ]:
C26H23Cl2N5O3
[ Molecular Weight ]:
524.402