| Bioactivity | GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. | ||||||||||||
| Target | EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR) | ||||||||||||
| Invitro | 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 µM[2]. | ||||||||||||
| Name | GLPG1837 | ||||||||||||
| CAS | 1654725-02-6 | ||||||||||||
| Formula | C16H20N4O3S | ||||||||||||
| Molar Mass | 348.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 ( [2]. Yeh HI, et al. A common mechanism for CFTR potentiators. J Gen Physiol. 2017 Dec 4;149(12):1105-1118. |
GLPG1837
CAS: 1654725-02-6 F: C16H20N4O3S W: 348.42
GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respecti
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