SB-435495 ditartrate_product_DataBase

Bioactivity	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].
Invitro	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]。 Western Blot Analysis[2] Cell Line:
In Vivo	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]。 Animal Model:
Name	SB-435495 ditartrate
CAS	304694-43-7
Formula	C46H52F4N6O14S
Molar Mass	1021.00
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
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.

PeptideDB

SB-435495 ditartrate

CAS: 304694-43-7 F: C46H52F4N6O14S W: 1021.00