GIBH-130
作者：齊岳
發(fā)布時(shí)間：2023-09-07
09:22:17
點(diǎn)擊數(shù)：
產(chǎn)品名稱：GIBH-130
產(chǎn)品描述：
| 產(chǎn)品描述 | GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation. |
| 靶點(diǎn)活性 | IL-1β:3.4 nM, NO:46.24 μM, TNF-α:40.82 μM |
| 體外活性 | GIBH-130 is a novel anti-neuroinflammatory 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. GIBH-130 has weak inhibition for NO (IC50: 46.24 μM) and TNF-α (IC50: 40.82 μM). Notably, pretreatment with GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50: 3.4 nM). The inhibitory efficiency of GIBH-130 (20 nM) is comparable to 20 μM minocycline against IL-1β release. IL-1β is one of the major cytokines during the neuroinflammatory progression of the AD [1]. |
| 體內(nèi)活性 | In both β amyloid-induced and APP/PS1 double transgenic Alzheimer's murine models, GIBH-130 (0.25 mg/kg) has comparable in vivo efficacy of cognitive impairment relief to donepezil and memantine respectively. As a potential drug candidate targeting in CNS, GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life. In addition, GIBH-130 displays good penetration ability across blood-brain barrier (AUCBrain/Plasma=0.21)[1]. |
| 分子量 | 360.41 |
| 分子式 | C20H20N6O |
| CAS No. | 1252608-59-5 |
存儲(chǔ)
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: Insoluble
DMSO: 10 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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