SB-435495

Names

[ Name ]:
SB-435495

[Synonym ]:
sb-435495
N-[2-(Diethylamino)ethyl]-2-{2-[(4-fluorobenzyl)sulfanyl]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4-oxo-1(4H)-pyrimidinyl}-N-{[4'-(trifluoromethyl)-4-biphenylyl]methyl}acetamide
1(4H)-Pyrimidineacetamide, N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-5-[(1-methyl-1H-pyrazol-4-yl)methyl]-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-

Biological Activity

[Description]:

SB-435495 is a potent, orally active inhibitor of Lp-PLA2 with IC50 of 0.06 nM; inhibits the enzyme in whole human plasma with IC50 of 3 nM; shows little interaction with other CYP450 enzymes (CYP450 IC50: 1A2>100 mM, 2C9>100 uM, 2C19>40 uM, 2D6=37 uM); effectively suppresses BRB breakdown in streptozotocin-diabetic Brown Norway rats,. Atherosclerosis Phase 2 Discontinued

[References]

References 1. Blackie JA, et al. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. 2. Canning P, et al. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7213-8. 3. Tyurin VA, et al. Cell Death Differ. 2014 May;21(5):825-35. 4. Jiang Z, et al. Respir Res. 2012 Nov 12;13:100. View Related Products by Target Phospholipase Atherosclerosis

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
793.9±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₈H₄₀F₄N₆O₂S

[ Molecular Weight ]:
720.822

[ Flash Point ]:
433.9±35.7 °C

[ Exact Mass ]:
720.286987

[ LogP ]:
7.48

[ Vapour Pressure ]:
0.0±2.8 mmHg at 25°C

[ Index of Refraction ]:
1.595

Related Compounds

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