Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GLPG1837 (ABBV-974) is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
説明 | GLPG1837 (ABBV-974) is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. |
ターゲット&IC50 | CFTR (G551D):339 nM (EC50), F508del CFTR:3 nM (EC50) |
In vitro | GLPG1837 increases the conductivity of the G551D CFTR channel with the obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with the apparent affinity within a range of 0.2~2 μM[2]. |
細胞研究 | CFBe41o- cells are cultured in Eagle's Minimal Essential Medium (MEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 1% l-glutamine, and 500 μg/mL hygromycin B. The cells are grown on culture flasks coated with 0.01% bovine serum albumin (BSA), 30 μg/mL Purecol, and 0.001% human fibronectin. CFBe41o- cells are transduced with adenoviruses containing F508del CFTR and YFP (H148Q/I152L/F47L). HEK293 cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin. HEK293 cells are transfected with plasmids containing G551D, G178R, S549N, R117H, CFTR, and YFP (H148Q/I152L/F47L). Directly after transfection, the HEK293 cells are seeded in black 96-well plates coated with poly-d-lysine at a density of 70000 cells per well. The next day, cells are incubated for 24 h at 27°C (CFBE41o?) or 37°C (HEK293). Then cells are treated for 10 min with 10 μM forskolin and the desired concentration of potentiator at room temperature. |
別名 | ABBV-974 |
分子量 | 348.42 |
分子式 | C16H20N4O3S |
CAS No. | 1654725-02-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (157.86 mM)
H2O: Insoluble
Ethanol: 5 mg/mL
You can also refer to dose conversion for different animals. 詳細
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GLPG1837 1654725-02-6 Autophagy Membrane transporter/Ion channel CFTR GLPG-1837 Cystic fibrosis transmembrane conductance regulator Inhibitor ABBV-974 inhibit GLPG 1837 ABBV974 ABBV 974 inhibitor