TrkA inhibitor compound 23（TrkA-IN-23）

Cas No.:	1821484-84-7
Chemical Name:	5-(2,4-dichloro-5-(pyridin-2-yl)benzamido)-N-(2-hydroxy-2-methylpropyl)-1-phenyl-1Hpyrazole-3-carboxamide
SMILES:	C1=CC=CC(C2=C(Cl)C=C(Cl)C(C(=O)NC3N(C4=CC=CC=C4)N=C(C(=O)NCC(C)(C)O)C=3)=C2)=N1
Formula:	C₂₆H₂₃Cl₂N₅O₃
M.Wt:	524.402
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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

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