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Azoramide

CAS No. : 932986-18-0

MCE 国际站：Azoramide

产品活性：Azoramide 是一种口服有效的未折叠蛋白反应 (UPR) 小分子调节剂。Azoramide 改善 ER 蛋白质折叠和提高 ER 伴侣能力，共同保护细胞免受 ER 应激。Azoramide 通过调节未折叠蛋白反应减轻 PLA2G6 突变体诱导的 ER 应激，并增强 CERB 信号以挽救线粒体功能，从而防止 DA 神经元凋亡 (apoptosis)。Azoramide 具有抗糖尿病活性。

研究领域：Apoptosis  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB

作用靶点：Apoptosis  |  Reactive Oxygen Species  |  Caspase  |  Bcl-2 Family  |  Mitochondrial Metabolism

In Vitro: Azoramide (0.01-100 µM; 0-24 h; Huh7 cells) regulates ER folding and secretion capacity without inducing ER stress.
Azoramide (15 µM; 2-16 h; Huh7 cells) protects cells from induced ER stress. Azoramide counteracts Tunicamycin (Tm, HY-A0098)-induced ATF6LD-Cluc secretion and Tm-induced decrease of ASGR-Cluc secretion. Azoramide suppresses Tm-induced GRP78 and CHOP protein expression.
Azoramide (15 µM; 2-16 h; Hepa 1-6 cells) alters ER calcium homeostasis and retains a greater fraction of Ca²⁺ in the ER.
Azoramide (0-10 µM; 5 d) attenuates loss of PLA2G6^D331Y/D331Y iPSC-derived midbrain DA neurons.
Azoramide (10 µM; 5 d) reduces the increase in ROS and ameliorates the decline in mitochondrial membrane potential in PLA2G6^D331Y/D331Y midbrain DA neurons.
Azoramide (10 µM; 0-30 d) suppresses mitochondrial fragmentation in PLA2G6^D331Y/D331Y midbrain DA neurons.

In Vivo: Azoramide (150 mg/kg; p.o.; daily, for 7 d; Huh7 cells; ob/ob mice) improves glucose homeostasis in mice with genetic obesity and preserves beta cell function and survival during metabolic ER stress.

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