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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $117 | In Stock | |
2 mg | $175 | In Stock | |
5 mg | $268 | In Stock | |
10 mg | $394 | In Stock | |
25 mg | $592 | In Stock | |
50 mg | $828 | In Stock | |
100 mg | Inquiry | In Stock | |
1 mL x 10 mM (in DMSO) | $323 | In Stock |
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. |
Targets&IC50 | DDR1:9.4 nM |
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]. |
Molecular Weight | 492.5 |
Formula | C26H23F3N6O |
Cas No. | 1934246-19-1 |
Smiles | C[C@@H]1C=2C(CN(C1)C=3C=NC=NC3)=CC(C(NC4=CC(=CC(C(F)(F)F)=C4)N5C=NC(C)=C5)=O)=CC2 |
Relative Density. | 1.37 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (101.52 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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