SB-435495 ditartrate 

SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA₂ inhibitor with an IC₅₀ of 0.06 nM^[1][3].

SB-435495 ditartrate 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) ditartrate 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^[2]。
SB-435495 (5 μM; 24-72 h) ditartrate 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SB-435495 (10 mg/kg; p.o.; once) ditartrate 抑制 WHHL 兔血浆 Lp-PLA₂ ^[1]。
SB-435495 (10 mg/kg; i.p.; daily for 28 days) ditartrate 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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1021.00

C₄₆H₅₂F₄N₆O₁₄S

304694-43-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]