Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family.
説明 | DDR-TRK-1 is a selective discoid domain receptor 1 (DDR1) inhibitor with IC50 value of 9.4 nM. DDR-TRK-1 also inhibits the TRK family. |
ターゲット&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. DDR-TRK-1 also exhibited reasonable pharmacokinetic (PK) properties. At an oral dose of 20 mg/kg in rats, the oral bioavailability was 66.8%, and the T1/2 value was 1.25 h. However, the area under the concentration-time curve (AUC) value of DDR-TRK-1 in mice was significantly higher than that in rats, indicating that its absorption performance in mice was good. By determining the binding affinity of DDR1-IN-3 and DDR1 protein, the inhibitory effect of DDR1 on DDR1-IN-3 can be further verified. The results show that DDR-TRK-1 is closely bound to DDR1, and the binding constant (Kd) value is 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]. |
分子量 | 492.5 |
分子式 | C26H23F3N6O |
CAS No. | 1934246-19-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (101.52 mM)
You can also refer to dose conversion for different animals. 詳細
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DDR-TRK-1 1934246-19-1 Tyrosine Kinase/Adaptors Discoidin Domain Receptor (DDR) DDRTRK1 DDR TRK 1 Inhibitor inhibitor inhibit