| Identification | Back Directory | [Name]
GIBH-130 | [CAS]
1252608-59-5 | [Synonyms]
GIBH-130
GIBH-130;GIBH 130;GIBH130
Methanone, (4-methyl-6-phenyl-3-pyridazinyl)[4-(2-pyrimidinyl)-1-piperazinyl]- | [Molecular Formula]
C20H20N6O | [MDL Number]
MFCD31544336 | [MOL File]
1252608-59-5.mol | [Molecular Weight]
360.41 |
| Chemical Properties | Back Directory | [Boiling point ]
664.5±65.0 °C(Predicted) | [density ]
1.268±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:50.0(Max Conc. mg/mL);138.73(Max Conc. mM)
Water:0.1(Max Conc. mg/mL);0.28(Max Conc. mM) | [form ]
Solid | [pka]
4.87±0.33(Predicted) | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC50=3.4 nM). | [in vivo]
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)[1]. | [IC 50]
IL-1β: 3.4 nM (IC50) | [References]
[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. DOI:10.1021/acschemneuro.6b00125 |
|
|