| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S87721-1mg买3赠1 |
99.80% | ￥230.00 |
9 | - | - | - | - |
|
S87721-5mg买3赠1 |
99.80% | ￥299.00 |
6 | - | - | - | - |
|
S87721-10mg买3赠1 |
99.80% | ￥460.00 |
5 | - | - | - | - |
|
S87721-25mg促销 |
99.80% | ￥690.00 ￥552.00 |
5 | - | - | - | - |
|
S87721-50mg促销 |
≥98% | ￥1100.00 ￥880.00 |
货期：2-3天 | - | - | - | - |
|
S87721-100mg促销 |
≥98% | ￥1990.00 ￥1590.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM). | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | IL-1β:3.4 nM (IC50);ILReceptor; TNF; Interleukin | ||||||||||||||||||||
| 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) | ||||||||||||||||||||
| 体内研究： | GIBH-130 exhibits comparable in vivo efficacy of cognitive impairment relief to donepezil and memantine respectively in both β amyloid-induced and APP/PS1 double transgenic Alzheimer’s murine models at a substantially lower dose (0.25 mg/kg). The pharmacokinetic properties of GIBH-130 are assessed in Sprague-Dawley rats. 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) | ||||||||||||||||||||
| 参考文献： | 1. Zhou W, et al. Microglia-Based Phenotypic Screening Identifies a Novel Inhibitor of Neuroinflammation Effective in Alzheimer's Disease Models. ACS Chem Neurosci. 2016 Nov 16;7(11):1499-1507. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京