1821484-84-7
1821484-84-7 structure
- Name: TrkA inhibitor compound 23(TrkA-IN-23)
- Chemical Name: TrkA-IN-23
- CAS Number: 1821484-84-7
- Molecular Formula: C26H23Cl2N5O3
- Molecular Weight: 524.402
- Create Date: 2020-01-19 15:06:30
- Modify Date: 2024-01-03 19:14:29
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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; 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.
| Name | TrkA-IN-23 |
|---|
| 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 |
| Molecular Formula | C26H23Cl2N5O3 |
|---|---|
| Molecular Weight | 524.402 |