GIBH-130
GIBH-130 Basic information
- Product Name:
- GIBH-130
- Synonyms:
-
- GIBH-130
- GIBH-130;GIBH 130;GIBH130
- Methanone, (4-methyl-6-phenyl-3-pyridazinyl)[4-(2-pyrimidinyl)-1-piperazinyl]-
- (4-methyl-6-phenyl-3-pyridazinyl)[4-(2-pyrimidinyl)-1-piperazinyl]-GIBH-130
- GIBH130,Inhibitor,Interleukin Related,GIBH 130,inhibit,GIBH-130
- 4-methyl-6-phenyl-3-[4-(pyrimidin-2-yl)piperazine-1-carbonyl]pyridazine
- GIBH-130, 10 mM in DMSO
- CAS:
- 1252608-59-5
- MF:
- C20H20N6O
- MW:
- 360.41
- Mol File:
- 1252608-59-5.mol
GIBH-130 Chemical Properties
- 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
GIBH-130 Usage And Synthesis
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
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