GLPG1837

GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR). It increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508 deletion (F508del) and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay. GLPG1837 increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a transepithelial clamp circuit (TECC) assay).Formal Name: N-[3-(aminocarbonyl)-4,7-dihydro-5,5,7,7-tetramethyl-5H-thieno[2,3-c]pyran-2-yl]-1H-pyrazole-3-carboxamide. CAS Number: 1654725-02-6. Synonyms: ABBV-974. Molecular Formula: C16H20N4O3S. Formula Weight: 348.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 226, 326 nm. SMILES: CC1(C)OC(C)(C)C2=C(C(C(N)=O)=C(NC(C3=NNC=C3)=O)S2)C1. InChi Code: 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). InChi Key: GHTGYZMBQPXTCQ-UHFFFAOYSA-N.