A CFTR potentiator; increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508del and G551D missense mutations with EC50 values of 88

GLPG1837 – 5 mg

Brand:
Cayman
CAS:
1654725-02-6
Storage:
-20
UN-No:
Non-Hazardous - /

GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).{52061,52059} 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).{52061}  

 

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SKU: 9003143 - 5 mg Category:

Description

A CFTR potentiator; increases forskolin-induced opening of wild-type and mutant CFTRs expressing the F508del and G551D missense mutations with EC50 values of 88, 3, and 339 nM, respectively, in a reporter assay; increases forskolin-induced conductivity of patient-derived bronchial epithelial cells expressing both F508del- and G551D-mutant CFTRs (EC50 = 159 nM in a 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

Synonyms:  ABBV-974

Molecular weight: 348.4

CAS: 1654725-02-6

Purity: ≥98%

Formulation: A crystalline solid

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