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FGIN-1-27

Cat. No. M6729
FGIN-1-27 Structure
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Biological Activity

FGIN-1-27 is a binds specifically and with high affinity to the peptide DBI receptor (benzodiazepine receptor) on mitochondrial membranes, inducing production of neurosteroids, which modulate GABA receptors (EC50 = 3 nM for increase in production of pregnenolone in glial cells). Thus it reduces anxiety without causing sedation.

Chemical Information
Molecular Weight 436.61
Formula C28H37FN2O
CAS Number 142720-24-9
Solubility (25°C) DMSO 43.66 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] Manera, et al. J Med Chem. Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists.

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