A CFTR potentiator
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GLPG1837

Item No. 9003143

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $213

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    10 mg

    $376

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    25 mg

    $820

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    Product Description

    GLPG1837 is a potentiator of cystic fibrosis transmembrane conductance regulator (CFTR).1,2 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).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gees, M., Musch, S., Van der Plas, S., et al. Identification and characterization of novel CFTR potentiators. Front. Pharmacol. 9, (2018).

    2. Van der Plas, S., Kelgtermans, H., De Munck, T., et al. Discovery of N‑(3-carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro‑4H‑thieno[2,3‑c]pyran-2-yl)‑lH‑pyrazole-5-carboxamide (GLPG1837), a novel potentiator which can open class III mutant cystic fibrosis transmembrane conductance regulator (CFTR) channels to a high extent. J. Med. Chem. 61(4), 1425-1435 (2018).