VU6015929

Research use only, not for human use.

VU6015929 is an inhibitor of active dual discoidin domain receptor 1/2 (DDR1/2)( IC50s of 4.67 nM and 7.39 nM, respectively).

VU6015929 is an inhibitor of active dual discoidin domain receptor 1/2 (DDR1/2)( IC50s of 4.67 nM and 7.39 nM, respectively).(In Vitro):VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.

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. 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 (CLp = 34.2 mL/min/kg), an ~3 hour half-life, moderate volume of distribution at steady state (Vss = 4.3 L/kg) and 12.5% oral bioavailability with a rapid Tmax (0.75 hr).

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Tyrosine Kinase

DDR

Endothelial lipase

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2442597-56-8

485.443

C24H19F4N5O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (515.01 mM)

Cn1ccc(n1)-c1cncc(CNc2cc(ccc2F)C(=O)Nc2cccc(OC(F)(F)F)c2)c1

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(-20℃)

With Ice Pack

≥ 2 years