Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]-
Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]- Basic information
- Product Name:
- Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]-
- Synonyms:
-
- Benzamide, 4-fluoro-3-[[[5-(1-methyl-1H-pyrazol-3-yl)-3-pyridinyl]methyl]amino]-N-[3-(trifluoromethoxy)phenyl]-
- 4-Fluoro-3-(((5-(1-methyl-1H-pyrazol-3-yl)pyridin-3-yl)methyl)amino)-N-(3-(trifluoromethoxy)phenyl)benzamide
- VU6015929,VU-6015929
- VU6015929, 10 mM in DMSO
- VU6015929 ，S6817
- CAS:
- 2442597-56-8
- MF:
- C24H19F4N5O2
- MW:
- 485.43
- Mol File:
- 2442597-56-8.mol
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.
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