GIBH-130

SKU: orb1302849

Description

GIBH-130 is a potent small molecule inhibitor of neuroinflammation, demonstrating high efficacy in suppressing IL-1β release from activated microglia with an IC50 of 3.4 nM. Its application is valuable for studying neuroinflammatory pathways in both cellular and animal models of neurological disorders.

Research Area

Cell Biology, Immunology & Inflammation

Key Properties

• CAS Number: 1252608-59-5
• MW: 360.41
• Purity: 99.86%
• Formula: C₂₀H₂₀N₆O
• SMILES: Cc1cc(nnc1C(=O)N1CCN(CC1)c1ncccn1)-c1ccccc1
• Target: IL Receptor,Interleukin,TNF
• Solubility: H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.55 mM);DMSO:27.5 mg/mL (76.3 mM)

Bioactivity

• Target IC50:
  NO:46.24 μM|IL-1β:3.4 nM|TNF-α:40.82 μM
• 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).
• 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 .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, IL-1β, ILReceptor, GIBH 130, GIBH130, GIBH-130, Interleukin Related, Interleukin, IL Receptor, TNF-α

Compound Identifiers

PubChem CID

50938773