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GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM. GLPG1837 shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor, the first marketed potentiator. GLPG1837 was generally safe and well tolerated in healthy subjects up to the highest dose of 800 mg twice daily for 2 weeks.
| Molecular Weight | 348.42 |
| Formula | C16H20N4O3S |
| CAS Number | 1654725-02-6 |
| Solubility (25°C) | DMSO: ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Yeh HI, et al. J Gen Physiol. A common mechanism for CFTR potentiators.
| Related CFTR Products |
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| GLPG2737
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. |
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