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
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
| Molecular Formula | C25H35NO5S |
| Molecular Weight | 461.614 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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.
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/29150844
Participants were treated with 200 mkL of GSK2981278 ointment (0.03%,
0.1%, 0.8% or 4%),
Route of Administration:
Topical
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:36:44 GMT 2025
by
admin
on
Mon Mar 31 18:36:44 GMT 2025
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| Record UNII |
L49V5G013I
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| Record Status |
Validated (UNII)
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300000041358
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1474110-21-8
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L49V5G013I
Created by
admin on Mon Mar 31 18:36:44 GMT 2025 , Edited by admin on Mon Mar 31 18:36:44 GMT 2025
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| Related Record | Type | Details | ||
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TARGET->INVERSE AGONIST |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |