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GIBH-130

GIBH-130
GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation.
Catalog No. T4450Cas No. 1252608-59-5
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Purity:99.86%
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GIBH-130

Catalog No. T4450Cas No. 1252608-59-5
GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation.
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
Pack SizePriceAvailabilityQuantity
1 mg$38In Stock
2 mg$54In Stock
5 mg$88In Stock
10 mg$155In Stock
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Product Introduction

Bioactivity
Description
GIBH-130 markedly inhibits the IL-1β secretion by activated microglia (IC50: 3.4 nM). GIBH-130 is an effective inhibitor of neuroinflammation.
Targets&IC50
IL-1β:3.4 nM, NO:46.24 μM, TNF-α:40.82 μM
In vitro
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].
In vivo
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].
Chemical Properties
Molecular Weight360.41
FormulaC20H20N6O
Cas No.1252608-59-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: Insoluble
DMSO: 27.5 mg/mL (76.3 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.7746 mL13.8731 mL27.7462 mL138.7309 mL
5 mM0.5549 mL2.7746 mL5.5492 mL27.7462 mL
10 mM0.2775 mL1.3873 mL2.7746 mL13.8731 mL
20 mM0.1387 mL0.6937 mL1.3873 mL6.9365 mL
50 mM0.0555 mL0.2775 mL0.5549 mL2.7746 mL

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