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GIBH-130

Cat. No. M9868
GIBH-130 Structure
Synonym:

GIBH130

Size Price Availability Quantity
10mg USD 185  USD185 In stock
25mg USD 400  USD400 In stock
50mg USD 620  USD620 In stock
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Quality Control & Documentation
Biological Activity

GIBH-130 is a neuroinflammation inhibitor, with IC50 value of 3.4 nM for suppressing the IL-1β secretion by activated microglia. GIBH-130 exhibited 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). GIBH-130 is found to be orally bioavailable in rats, with 74.91% bioavailability and 4.32 h half-life.

Chemical Information
Molecular Weight 360.41
Formula C20H20N6O
CAS Number 1252608-59-5
Solubility (25°C) DMSO 44 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wei Zhou, et al. ACS Chem Neurosci. Microglia-Based Phenotypic Screening Identifies a Novel Inhibitor of Neuroinflammation Effective in Alzheimer's Disease Models

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