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GLPG2451

Cat. No. M21104
GLPG2451  Structure
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Biological Activity

GLPG2451 is an enhancer of cystic fibrosis transmembrane conductance regulator (CFTR) and effectively enhances cryo-rescued F508del CFTR with an EC50 of 11.1 nM.

Chemical Information
Molecular Weight 419.38
Formula C16H16F3N3O5S
CAS Number 2055015-61-5
Solubility (25°C) DMSO ≥ 200 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] Steven E Van der Plas, et al. J Med Chem. Correction to "Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis"

[2] Steven E Van der Plas, et al. J Med Chem. Discovery of GLPG2451, a Novel Once Daily Potentiator for the Treatment of Cystic Fibrosis

[3] Maarten Gees, et al. Front Pharmacol. Identification and Characterization of Novel CFTR Potentiators

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