ThioLox

ThioLox is a competitive 15-lipoxygenase-1 (15-LOX-1) inhibitor with a Ki of 3.30 μM. ThioLox shows anti-inflammatory and neuroprotective properties[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> 5-Lipoxygenase

Research Areas >> Neurological Disease

Ki: 3.30 μM (15-LOX-1)[1]

ThioLox (50 μM; 24 h) 抑制精确切肺切片 (PCLS) 中白细胞介素 (IL-1β, IL-6, IL-8, IL-12b, TNFα 和 iNOS) 的表达[1]。 ThioLox (10 μM; 16 h) 在神经元细胞中防止脂质过氧化和线粒体超氧化物的形成[1]。 ThioLox (5-20 μM; 14-16 h) 保护 HT-22 细胞免受谷氨酸毒性，显著降低神经元细胞死亡[1]。 RT-PCR[1] Cell Line: Precision-cut lung slices (PCLS) Concentration: 1, 5, 10, 25 and 50 μM Incubation Time: In combination with 10 μM linoleic acid for 20 h and stimulated with 10 ng/mL LPS for the last 4 h. Result: Provided almost 50% inhibition of the expression of the pro-inflammatory genes IL-1β, IL-6, IL-8, IL-12b, TNFα and iNOS at 50 μM. Cell Viability Assay[1] Cell Line: Neuronal HT-22 cells Concentration: 5, 10 and 20 μM Incubation Time: 14-16 h Result: Significantly reduced neuronal cell death against glutamate toxicity.

ThioLox 的 logP 值为 3，测得的数值预测能透过血脑屏障[1]。

[1]. Eleftheriadis N, et al. Design of a novel thiophene inhibitor of 15-lipoxygenase-1 with both anti-inflammatory and neuroprotective properties. Eur J Med Chem. 2016 Oct 21;122:786-801.