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;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
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)
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..…
N-Bromosuccinimide Price
- Product number
- 20974
- Product name
- GSK2981278
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $37
- Updated
- 2024/03/01
- Product number
- 20974
- Product name
- GSK2981278
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- 20974
- Product name
- GSK2981278
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $283
- Updated
- 2024/03/01
- Product number
- 20974
- Product name
- GSK2981278
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $618
- Updated
- 2024/03/01
- Product number
- C3707
- Product name
- GSK2981278
- Packaging
- 25mg
- Price
- $705
- Updated
- 2021/12/16
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
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