An inverse agonist of RORγ
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GSK2981278

Item No. 20974

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide
CAS Number
1474110-21-8
Molecular Formula
C25H35NO5S
Formula Weight
461.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 5 mg/mlEthanol: 15 mg/ml
λmax
246 nm
SMILES
OCC1=CC(S(N(CC(C)C)C2=CC=C(CC)C=C2)(=O)=O)=CC=C1OCC3CCOCC3
InChi Code
InChI=1S/C25H35NO5S/c1-4-20-5-7-23(8-6-20)26(16-19(2)3)32(28,29)24-9-10-25(22(15-24)17-27)31-18-21-11-13-30-14-12-21/h5-10,15,19,21,27H,4,11-14,16-18H2,1-3H3
InChi Key
LZLBRISQTJVZNP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $312

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    25 mg

    $680

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    Product Description

    GSK2981278 is an inverse agonist of retinoic acid receptor-related nuclear receptor γ (RORγ; IC50 = 17 nM in a transactivation assay).1 It is selective for RORγ over RORα.2 GSK2981278 inhibits IL-17A and IL-22 protein secretion from isolated human peripheral blood T cells grown under Th17 skewing conditions (IC50 = 3.2 nM). Topical application of GSK2981278 (1% ointment) reduces dermal symptoms in a mouse model of psoriasis induced by imiquimod (Item No. 14956).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ouvry, G., Bihl, F., Bouix-Peter, C., et al. Sulfoximines as potent RORγ inverse agonists. Bioorg. Med. Chem. Lett. 28(8), 1269-1273 (2018).

    2. Smith, S.H., Peredo, C.E., Takedo, Y., et al. Development of a topical treatment for psoriasis targeting RORγ: From bench to skin. PLoS One 11(2), e0147979 (2016).