GLPG-1837

SKU: orb1225994

Description

GLPG-1837 (ABBV-974) is a potent, orally available CFTR potentiator with EC50 of 3 nM and 339 nM on F508del and G551D CFTR, respectively; shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor.Cystic Fibrosis,Phase 2 Clinical(In Vitro):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 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2～2 μM.

Key Properties

• CAS Number: 1654725-02-6
• MW: 348.421
• Purity: >98% (HPLC)
• Formula: C₁₆H₂₀N₄O₃S
• SMILES: O=C(C1=NNC=C1)NC(S2)=C(C(N)=O)C3=C2C(C)(C)OC(C)(C)C3
• Target: CFTR
• Solubility: Ethanol: 5 mg/mL; Water: Insoluble; DMSO: 60 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  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 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2~2 μM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GLPG1837 | GLPG 1837 | ABBV-974

Quick Database Links

Gene Symbol

CFTR