Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C19H28BN3O5.2ClH |
| Molecular Weight | 462.176 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.NCCN[C@H]1CC[C@H](CC(=O)N[C@H]2CC3=CC=CC(C(O)=O)=C3OB2O)CC1
InChI
InChIKey=CKWIMFZHNCBHIX-DKZBTPFISA-N
InChI=1S/C19H28BN3O5.2ClH/c21-8-9-22-14-6-4-12(5-7-14)10-17(24)23-16-11-13-2-1-3-15(19(25)26)18(13)28-20(16)27;;/h1-3,12,14,16,22,27H,4-11,21H2,(H,23,24)(H,25,26);2*1H/t12-,14-,16-;;/m0../s1
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
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
HI-20
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY | |||
|
100000183477
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY | |||
|
C171699
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY | |||
|
137331954
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY | |||
|
4VND3V607A
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY | |||
|
2244235-49-0
Created by
admin on Tue Apr 01 19:31:11 GMT 2025 , Edited by admin on Tue Apr 01 19:31:11 GMT 2025
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD