304694-39-1

304694-39-1 structure

Name: SB-435495
Chemical Name: sb-435495
CAS Number: 304694-39-1
Molecular Formula: C₃₈H₄₀F₄N₆O₂S
Molecular Weight: 720.822
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phospholipase
Create Date: 2020-01-20 18:14:57
Modify Date: 2024-01-11 19:28:42
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

Name	sb-435495
Synonyms	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]-

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