GLPG2737 is a novel potent Type 2 corrector of CFTR. GLPG2737 showed high permeability both in MDCKII-MDRI and Caco-2 cells, with low efflux allowing an elevated absorbed fraction FaxFg and a dose proportional increase in exposure in rat from a dose of 5 to 300 mg/kg, despite a low aqueous thermodynamic solubility. GLPG2737 was found to only inhibit binding from cognate radioligands to (h)H1 and (h)Sigma with respective IC50s determined to be 8 and 0.36 μM.
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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