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| | Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- Basic information |
| | Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- Chemical Properties |
| Boiling point | 553.3±50.0 °C(Predicted) | | density | 1.37±0.1 g/cm3(Predicted) | | solubility | Soluble to 100 mM in DMSO and to 20 mM in ethanol | | pka | 12.62±0.70(Predicted) | | form | Solid | | color | White to yellow |
| | Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- Usage And Synthesis |
| Uses | 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]. | | 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]. | | IC 50 | DDR1: 4.67 nM (IC50); DDR2: 7.39 nM (IC50) | | storage | Store at -20°C | | References | [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. |
| | Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- Preparation Products And Raw materials |
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