SB-435495

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB-435495 是一种有效的、口服活性的 Lp-PLA2 抑制剂，IC50 为 0.06 nM。

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.

Western Blot Analysis Cell Line:oxLDL-exposed human umbilical vein endothelial cells Concentration:5 μM Incubation Time:24 hResult:The expression of Lp-PLA2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172).Cell Viability Assay Cell Line:oxLDL-exposed human umbilical vein endothelial cells Concentration:5 μM Incubation Time:24, 48 and 72 h Result:Significantly increased cell viability.

——

SB435495

Metabolic Enzyme/Protease

Phospholipase

Phospholipase

Cardiovascular Disease

Atherosclerosis

304694-39-1

720.832

C38H40F4N6O2S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (138.73 mM)

CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C=C(C(=O)N=C3SCC4=CC=C(C=C4)F)CC5=CN(N=C5)C

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]-

(-20℃)

With Ice Pack

≥ 2 years