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GIBH-130

Catalog No. T4450 CAS 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.

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GIBH-130, CAS 1252608-59-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 88.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 343.00
50 mg	In stock	$ 563.00
100 mg	In stock	$ 773.00
1 mL * 10 mM (in DMSO)	In stock	$ 107.00

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Purity: 99.86%

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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].

Molecular Weight	360.41
Formula	C20H20N6O
CAS No.	1252608-59-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 27.5 mg/mL (76.3 mM), Sonication is recommended.

References and Literature

1. Zhou W, Zhong G, Fu S, et al. Microglia-Based Phenotypic Screening Identifies a Novel Inhibitor of Neuroinflammation Effective in Alzheimer's Disease Models[J]. Acs Chemical Neuroscience, 2016, 7(11):1499-1507.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Immuno-Oncology Compound Library Bioactive Compound Library Apoptosis Compound Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library HIF-1 Signaling Pathway Compound Library Pyroptosis Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

GIBH-130 1252608-59-5 Apoptosis Immunology/Inflammation Interleukin TNF IL Receptor Inhibitor Interleukin Related GIBH 130 inhibit GIBH130 inhibitor

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