消旋-7-氧代普拉克索 T26326

Product Introduction
Bioactivity


英文名: VU0285655-1

描述: VU0285655-1(BML-280) 是一种有效的选择性磷脂酶 D2 (PLD2) 抑制剂，可抑制PLD2 缺陷细胞的增殖。VU0285655-1 对高糖诱导的 caspase-3 裂解和细胞活力降低有抑制作用。VU0285655-1 可用于研究糖尿病视网膜病。

体外活性: VU0285655-1 (BML-280) (0-5 µM; 24 h; Wild-type, PLD1- and PLD2-deficient astrocytes) reduces proliferation in PLD1-deficient cells, but also in PLD2-deficient cells exposed to IGF-1. BML-280 had minor effects in wild-type and PLD2-deficient cells but completely blocked PLD activity in PLD1-deficient cells. Caused a highly significant inhibition of glial proliferation when astrocytes were stimulated by FCS (fetal calf serum) or IGF-1, respectively. Showed non-specific effects because they inhibited cell proliferation even in PLD1/2 double knockouts at 5 µM.[1]BML-280 inhibits mRNA levels and secretion of tumor necrosis factor-α, IL-1β and IL-8 in human periodontal ligament cells.[2]VU0285655-1 shows an approximately 21-fold selectivity for PLD2.[3]BML-280 (0-0.1 µM) suppresses formyl-Met-Leu-Phe (fMLP)-stimulated PLD activity in a concentration-dependent manner, with an IC50 of 0.04 ± 0.01 μM.[3]BML-280 (0-0.3 µM) inhibits O2- generation, and the inhibition reaches a plateau (about 20 % inhibition) at around 0.01 μM to 0.3 μM.[3]

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (116.41 mM)


关键字: VU0285655-1

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相关库: Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途