For research use only. Not for therapeutic Use.
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].
SB-435495 inhibits CYP450 3A4 with an IC50 of 10 μM and the black membrane permeability is 0.017 cm/h[1].
SB-435495 (5 μM; 24 h) significantly inhibits the expression of Lp-PLA2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs[2].
SB-435495 (5 μM; 24-72 h) significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs[2].
SB-435495 (10 mg/kg; p.o.; once) inhibits plasma Lp-PLA2 in the WHHL rabbit[1].
SB-435495 (10 mg/kg; i.p.; daily for 28 days) effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin (HY-13753)-diabetic Brown Norway rats[3].
| Catalog Number | I041267 |
| CAS Number | 304694-39-1 |
| Synonyms | N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-5-[(1-methylpyrazol-4-yl)methyl]-4-oxopyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide |
| Molecular Formula | C38H40F4N6O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C38H40F4N6O2S/c1-4-46(5-2)18-19-47(23-27-6-10-30(11-7-27)31-12-14-33(15-13-31)38(40,41)42)35(49)25-48-24-32(20-29-21-43-45(3)22-29)36(50)44-37(48)51-26-28-8-16-34(39)17-9-28/h6-17,21-22,24H,4-5,18-20,23,25-26H2,1-3H3 |
| InChIKey | VGIQUSQBXZXBGW-UHFFFAOYSA-N |
| SMILES | 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 |
| Reference | [1]. Blackie JA, et al. The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. [2]. Yang L, et al. AMP-activated protein kinase mediates the effects of lipoprotein-associated phospholipase A2 on endothelial dysfunction in atherosclerosis. Exp Ther Med. 2017 Apr;13(4):1622-1629. [3]. Canning P, et al. Lipoprotein-associated phospholipase A2 (Lp-PLA2) as a therapeutic target to prevent retinal vasopermeability during diabetes. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7213-8. |
