GLPG1837

SKU: orb1300090

Description

GLPG1837

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1654725-02-6
• MW: 348.42
• Purity: 99.73%
• Formula: C₁₆H₂₀N₄O₃S
• SMILES: CC1(C)Cc2c(sc(NC(=O)c3cc[nH]n3)c2C(N)=O)C(C)(C)O1
• Target: CFTR,Autophagy
• Solubility: Ethanol:5 mg/mL (14.35 mM);DMSO:55 mg/mL (157.86 mM);H2O:Insoluble

Bioactivity

• Target 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. GLPG1837 is reversible CFTR potentiator, with the apparent affinity within a range of 0.2～2 μM.
• Cell Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GLPG1837, GLPG-1837, GLPG 1837, Inhibitor, inhibit, ABBV 974, ABBV974, ABBV-974, Autophagy, Cystic fibrosis transmembrane conductance regulator, CFTR

Compound Identifiers

PubChem CID

117857370