| Description | SB-435495 is an orally active, selective and potent Lp-PLA2 inhibitor (IC50: 0.06 nM) for the study of autoimmune uveitis and atherosclerosis. |
| In vitro | SB-435495 抑制 CYP450 3A4 的 IC50 为 10 μM，膜通透性为 0.017 cm/h[1];SB-435495 (5 μM; 24 h) 显著抑制 Lp-PLA2 蛋白的表达，同时提高 oxLDL 暴露 HUVECs 中 AMPKα 和磷酸化-AMPKα (T172) 的表达水平;SB-435495 (5 μM; 24-72 h) 在 oxLDL 暴露 HUVECs 中显著增加细胞活力和 NO 表达，显著降低 ET-1 表达[2]。 |
| In vivo | SB-435495 (10 mg/kg; p.o.; once) 抑制 WHHL 兔血浆 Lp-PLA2 [1]。SB-435495 (10 mg/kg; i.p.; daily for 28 days) 在 Streptozotocin (HY-13753) 糖尿病褐挪威大鼠中有效抑制血视网膜屏障 (BRB) 的破坏[3]。 |
| Synonyms | SB435495, SB 435495 |
| molecular weight | 720.82 |
| Molecular formula | C38H40F4N6O2S |
| CAS | 304694-39-1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (110.98 mM), Sonication is recommended. |
| References | 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. |