| Name | DDR-TRK-1 |
| Description | DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family. |
| In vitro | DDR-TRK-1 is a promising candidate with an IC50 value of 9.4 nM relative to DDR1. It exhibited reasonable pharmacokinetic (PK) properties, with an oral bioavailability of 66.8% and a T1/2 value of 1.25 h at a 20 mg/kg oral dose in rats. The area under the concentration-time curve (AUC) value in mice was significantly higher than in rats, indicating good absorption performance in mice. Binding affinity studies of DDR1-IN-3 and DDR1 protein further verified DDR-TRK-1's inhibitory effect on DDR1, showing a binding constant (Kd) value of 4.7 nM[1]. |
| In vivo | DDR-TRK-1 can prevent blm-induced pathological changes in a dose-dependent manner. These results agree with the expression levels of fibrosis markers in the lung tissue, including lysates, including fibronectin and α-smooth muscle actin (SMA). Further analysis also showed that the use of DDR-TRK-1 resulted in a dose-dependent inhibition of hydroxyproline content, a unique amino acid found in collagen. The above data indicate that DDR-TRK-1 has good therapeutic potential for blm-induced pulmonary fibrosis[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (101.52 mM), Sonication is recommended.
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| Keywords | DiscoidinDomainReceptor(DDR) | DiscoidinDomainReceptor | Discoidin Domain Receptor (DDR) | Discoidin Domain Receptor | DDR-TRK-1 | DDRTRK1 | DDR1 | DDR TRK 1 | DDR |
| Inhibitors Related | DDR Inhibitor | Ddr1-In-1 | VU6015929 | DDR1-IN-4 | FGFR1/DDR2 inhibitor 1 | WRG-28 | Sitravatinib | LCB 03-0110 | DDR1-IN-2 | Merestinib | (S)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-2-(pyrimidin-5-yl)-1,2,3,4-tetrahydroisoquinoline-7-carboxamide |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library |
United States
