VU6015929 用途与合成方法
| Target | Value |
|
DDR1
(Cell-free assay) | 4.67 nM |
|
DDR2
(Cell-free assay) | 7.39 nM |
VU6015929 (Compound 7e; 4-100 nM; 24 hours; HEK293-DDR1b cells) treatment inhibits collagen I-induced DDR1 phosphorylation in a dose dependent manner. Analysis of the phosphorylated DDR1/total DDR1 ratio reveals an IC 50 for VU6015929 of 0.7078 nM.
Western Blot Analysis
| Cell Line: | HEK293-DDR1b cells |
| Concentration: | 4 nM, 20 nM, 100 nM |
| Incubation Time: | 24 hours |
| Result: | Inhibited collagen I-induced DDR1 phosphorylation in a dose dependent manner. Significantly inhibited collagen IV production. |
VU6015929 (Compound 7e) is further evaluated in a rat IV (0.5 mg/kg)/PO (3 mg/kg) PK study in a 10% EtOH/40% PEG400/50% saline vehicle. VU6015929 displays a good in vitro:in vivo correlation (IVIC), with moderate in vivo clearance (CL p = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (V ss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid T max (0.75 hr).
