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VU6015929

CAS No. : 2442597-56-8

产品活性：VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC₅₀s of 4.67 nM and 7.39 nM, respectively. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production.

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Discoidin Domain Receptor

In Vitro: 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 IC₅₀ for VU6015929 of 0.7078 nM.

In Vivo: 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).

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