GIBH-130CAS号: 1252608-59-5分子式: C20H20N6O分子量: 360.41描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM).
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
可溶性/溶解性 |
DMSO : 50 mg/mL (138.73 mM; Need ultrasonic)
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生物活性 | |
In vitro(体外研究) |
GIBH-130 is a novel antineuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC50 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. The IC50 values of GIBH-130 for NO and TNF-α inhibition are 46.24 and 40.82 μM, respectively. Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM). The inhibitory efficiency of GIBH-130 at 20 nM is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during neuroinflammatory progression of AD. So, it is meaningful to explain the selectivity of GIBH-130 against IL-1β (IC50 value 3.4 nM) over NO and TNF-α (IC50 value 46.24 and 40.82 μM, respectively) .
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In vivo(体内研究) |
GIBH-130 is a novel antineuroinflammatory agent that is identified through microglia-based phenotypic screenings. GIBH-130 (IC50 3.4 nM) is identified in screenings as one of the most effective inhibitors with an acceptable half-life. Pretreatment of microglia with GIBH-130 significantly reduces the production of these factors in response to Lipopolysaccharides (LPS) stimulation, and the extent of the reduction is dependent on the concentrations of GIBH-130. The IC50 values of GIBH-130 for NO and TNF-α inhibition are 46.24 and 40.82 μM, respectively. Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM). The inhibitory efficiency of GIBH-130 at 20 nM is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during neuroinflammatory progression of AD. So, it is meaningful to explain the selectivity of GIBH-130 against IL-1β (IC50 value 3.4 nM) over NO and TNF-α (IC50 value 46.24 and 40.82 μM, respectively) .
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分子结构图