GLPG1837 (Synonyms: ABBV-974) |
| Catalog No.GC19169 |
GLPG1837 es un potenciador CFTR potente y reversible, con EC50 de 3 nM y 339 nM para F508del y G551D CFTR, respectivamente.
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Cas No.: 1654725-02-6
Sample solution is provided at 25 µL, 10mM.
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GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
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[1]. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2∼2 uM[2].
References:
[1]. Van der Plas SE, et al. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent. J Med Chem. 2018 Feb 22;61(4):1425-1435.
[2]. Yeh HI, et al. A common mechanism for CFTR potentiators. J Gen Physiol. 2017 Dec 4;149(12):1105-1118.
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