| Identification | Back Directory | [Name]
Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- | [CAS]
2442597-56-8 | [Synonyms]
VU6015929,VU-6015929
4-Fluoro-3-(((5-(1-methyl-1H-pyrazol-3-yl)pyridin-3-yl)methyl)amino)-N-(3-(trifluoromethoxy)phenyl)benzamide
Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- | [Molecular Formula]
C24H19F4N5O2 | [MDL Number]
MFCD32667038 | [MOL File]
2442597-56-8.mol | [Molecular Weight]
485.43 |
| Chemical Properties | Back Directory | [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 | [form ]
Solid | [pka]
12.62±0.70(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [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. |
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