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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $117 | In Stock | In Stock | |
| 2 mg | $175 | In Stock | In Stock | |
| 5 mg | $268 | In Stock | In Stock | |
| 10 mg | $394 | In Stock | In Stock | |
| 25 mg | $592 | In Stock | In Stock | |
| 50 mg | $828 | In Stock | In Stock | |
| 100 mg | Preferential | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $323 | In Stock | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (101.52 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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