GLPG1837

• CAT Number: I014394
• CAS Number: 1654725-02-6
• Molecular Formula: C16H20N4O3S
• Molecular Weight: 348.42
• Purity: ≥95%
• Solubility: Soluble in DMSO
• IUPAC Name: N-(3-carbamoyl-5,5,7,7-tetramethyl-4H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-5-carboxamide
• InChI: InChI=1S/C16H20N4O3S/c1-15(2)7-8-10(12(17)21)14(24-11(8)16(3,4)23-15)19-13(22)9-5-6-18-20-9/h5-6H,7H2,1-4H3,(H2,17,21)(H,18,20)(H,19,22)
• InChIKey: GHTGYZMBQPXTCQ-UHFFFAOYSA-N
• SMILES: O=C(C1=NNC=C1)NC(S2)=C(C(N)=O)C3=C2C(C)(C)OC(C)(C)C3

GLPG-1837 (Cat.No:I014394), also known as ABBV-974, is a novel cystic fibrosis transmembrane conductance regulator (CFTR) potentiator1. GLPG1837 was generally safe and well tolerated in healthy subjects up to the highest dose of 800 mg twice daily for 2 weeks. GLPG1837 shows enhanced efficacy on CFTR mutants harboring Class III mutations compared to Ivacaftor, the first marketed potentiator.

Reference

Cystic fibrosis (CF) is caused by mutations in the gene for the cystic fibrosis transmembrane conductance regulator (CFTR). With the discovery of Ivacaftor and Orkambi, it has been shown that CFTR function can be partially restored by administering one or more small molecules. These molecules aim at either enhancing the amount of CFTR on the cell surface (correctors) or at improving the gating function of the CFTR channel (potentiators).