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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 |
|---|
| Ataluren
Ataluren (PTC124) is a novel, orally available small molecular CFTR-G542X nonsense allele inhibitor. |
| VX-770 (Ivacaftor)
VX-770 (Ivacaftor) is a first-in-class potentiator of CFTR, which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. |
| Lonidamine
Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). |
| VX-809
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell. |
| CFTR(inh)-172
CFTR(inh)-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. |
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