ChemicalBook > CAS DataBase List > N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide

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

Product Name
N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide
CAS No.
1474110-21-8
Chemical Name
N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide
Synonyms
CS-2157;GSK2981278;ROR gamma GS2981278;ROR gama modulator 1;GSK-2981278;GSK 2981278;ROR GAMA MODULATOR 1;N-(4-Ethyl-phenyl)-3-hydroxymethyl-N-isobutyl-4-(tetrahydro-pyran-4-ylmethoxy)-benzenesulfonamide;N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide;N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide;Benzenesulfonamide, N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-;IL-22,ointment,RAR-related orphan receptor,psoriasis,topically,GSK2981278,GSK 2981278,inflammation,il17,inverse,binding,IL-17A,ROR,inhibit,RORγ-DNA,Inhibitor,GSK-2981278
CBNumber
CB43037591
Molecular Formula
C25H35NO5S
Formula Weight
461.61
MOL File
1474110-21-8.mol
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N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide Property

Boiling point:
622.6±65.0 °C(Predicted)
Density 
1.180±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≤15mg/ml in ethanol;5mg/ml in DMSO;30mg/ml in dimethyl formamide
form 
crystalline solid
pka
14.10±0.10(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
20974
Product name
GSK2981278
Purity
≥98%
Packaging
1mg
Price
$37
Updated
2024/03/01
Cayman Chemical
Product number
20974
Product name
GSK2981278
Purity
≥98%
Packaging
5mg
Price
$161
Updated
2024/03/01
Cayman Chemical
Product number
20974
Product name
GSK2981278
Purity
≥98%
Packaging
10mg
Price
$283
Updated
2024/03/01
Cayman Chemical
Product number
20974
Product name
GSK2981278
Purity
≥98%
Packaging
25mg
Price
$618
Updated
2024/03/01
ApexBio Technology
Product number
C3707
Product name
GSK2981278
Packaging
25mg
Price
$705
Updated
2021/12/16
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N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide Chemical Properties,Usage,Production

Biological Activity

gsk2981278 is a rorγ-selective inverse agonist.rar-related orphan receptor gamma (rorγ) is a protein that in humans is encoded by the rorc gene. the rorγ protein is a dna-binding transcription factor and is a member of the nr1 subfamily of nuclear receptors.

in vitro

previous study found that gsk2981278 had no significant effect on rorα-dependent activation, indicating its selectivity for rorγ. gsk2981278 also demonstrated 10-fold greater potency for il-17a inhibition than its analogs of gsk3038548 and gsk3038549. in addition, authors examined the effect of gsk2981278 on endogenous il17a expression in jurkat cells. results showed that gsk2981278 could repress the activation of il17a by rorγt in a dose-responsive manner [1].

in vivo

in previous study, the imiquimod (imq) mouse model was employed to demonstrate efficacy of gsk2981278 in a psoriaform-like mouse model. results showed that the topical application of imq could induce and exacerbate psoriasis-like chronic skin inflammation in mice. next, mice were treated topically with gsk2981278 for three days, after which mice continued to receive compound for the duration of the study. it was found that gsk2981278 was undetectable in serum at harvest, suggesting that systemic exposure was minimal. in addition, mice exposed to gsk2981278 exhibited reduced skin redness and scaling, as well as decreased hyperplasia [1].

References

[1] smith sh et al. development of a topical treatment for psoriasis targeting rorγ: from bench to skin. plos one. 2016 feb 12;11(2):e0147979.
[2] https://clinicaltrials. gov/ct2/show/nct02548052 term=gsk2981278&rank=2

N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide Preparation Products And Raw materials

Raw materials

Preparation Products

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

MedChemexpress LLC
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1474110-21-8, N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamideRelated Search:


  • ROR gamma GS2981278
  • CS-2157
  • N-(4-Ethyl-phenyl)-3-hydroxymethyl-N-isobutyl-4-(tetrahydro-pyran-4-ylmethoxy)-benzenesulfonamide
  • N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide
  • ROR gama modulator 1
  • GSK2981278
  • GSK-2981278;GSK 2981278;ROR GAMA MODULATOR 1
  • Benzenesulfonamide, N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-
  • IL-22,ointment,RAR-related orphan receptor,psoriasis,topically,GSK2981278,GSK 2981278,inflammation,il17,inverse,binding,IL-17A,ROR,inhibit,RORγ-DNA,Inhibitor,GSK-2981278
  • N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-[(tetrahydro-2H-pyran-4-yl)methoxy]-benzenesulfonamide
  • 1474110-21-8