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Details

Stereochemistry ACHIRAL
Molecular Formula C25H35NO5S
Molecular Weight 461.614
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of GSK-2981278

SMILES

CCC1=CC=C(C=C1)N(CC(C)C)S(=O)(=O)C2=CC(CO)=C(OCC3CCOCC3)C=C2

InChI

InChIKey=LZLBRISQTJVZNP-UHFFFAOYSA-N
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

HIDE SMILES / InChI

Molecular Formula C25H35NO5S
Molecular Weight 461.614
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

N-(4-Ethylphenyl)-3-(Hydroxymethyl)-N-Isobutyl-4-(Tetrahydro-2h-Pyran-4-Ylmethoxy)Benzenesulfonamide (also known as GSK2981278) is a highly potent and selective inverse agonist of RORγ under development for the topical treatment of psoriasis. Preclinical data showed that GSK2981278 significantly inhibited the production of the Th17 signature cytokines in multiple in vitro and human tissue‐based systems. GSK2981278 may block the transcriptional activity of RORγt, leading to local suppression of cytokine expression and ultimately, improvement in psoriasis. Unfortunately in phase I clinical trial clinical assessment results showed no improvement of psoriatic lesions following treatment with GSK2981278.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Participants were treated with 200 mkL of GSK2981278 ointment (0.03%, 0.1%, 0.8% or 4%),
Route of Administration: Topical
Substance Class Chemical
Record UNII
L49V5G013I
Record Status Validated (UNII)
Record Version