Catalog No. size PriceQuantity
M6485-2 2mg solid $128
M6485-10 10mg solid $510


GSK-2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). GSK-2981278 is a strong RORγ-selective inverse agonist that inhibits activation of the il17 promoter. GSK-2981278 robustly inhibits RORγ-mediated cytokine production at both the mRNA and protein level. GSK-2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK-2981278 will significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients.

Product information

CAS Number: 1474110-21-8

Molecular Weight: 461.61

Formula: C25H35NO5S


GSK 2981278



Chemical Name: N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide

Smiles: CC(C)CN(C1=CC=C(CC)C=C1)S(=O)(=O)C1=CC(CO)=C(C=C1)OCC1CCOCC1


InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GSK-2981278 markedly and potently inhibits IL-17A and IL-22 protein secretion in a concentration dependent manner (IC50 = 3.2 nM) during 5 days of culture under Th17 skewing conditions. GSK-2981278 (0.3, 1, 3, 10, 30, 100, 300, 1000 pM; 5 day) potently and selectively inhibits IL-17 and IL-22 levels. Culture in the presence of ≥3 nM GSK-2981278 led to a near-complete inhibition of IL-17A protein secretion.

In Vivo:

GSK-2981278 (1% in ointment; topically; for three days) reduces skin redness and scaling, as well as decreased hyperplasia, as evidenced by a 23% reduction in epidermal thickness. GSK-2981278 attenuates inflammation in a mouse model of psoriasis.


  1. Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM, Birault V, Viviani F, Hofland H, Jetten AM, Cote-Sierra J. Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. PLoS One. 2016 Feb 12;11(2):e0147979. doi: 10.1371/journal.pone.0147979. PubMed PMID: 26870941; PubMed Central PMCID: PMC4752338.

Products are for research use only. Not for human use.

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed