| Bioactivity | 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[1]. | ||||||||||||
| Invitro | 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[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| 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 (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)[1]. | ||||||||||||
| Name | VU6015929 | ||||||||||||
| CAS | 2442597-56-8 | ||||||||||||
| Formula | C24H19F4N5O2 | ||||||||||||
| Molar Mass | 485.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Daniel E. Jeffries, et al. Discovery of VU6015929: A Selective Discoidin Domain Receptor 1/2 (DDR1/2) Inhibitor to Explore the Role of DDR1 in Antifibrotic Therapy. ACS Med. Chem. Lett. 2019. |
VU6015929
CAS: 2442597-56-8 F: C24H19F4N5O2 W: 485.43
VU6015929 is a potent, selective and orally active dual discoidin domain receptor 1/2 (DDR1/2) inhibitor with IC50s of 4
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