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GSK2981278 - 98%, high purity , CAS No.1474110-21-8, Agonist of RAR-related orphan receptor-γ

Moligand™
≥98%

CAS#: 1474110-21-8
Formula: C₂₅H₃₅NO₅S
Molecular Weight: 461.61
PubChem CID: 89875987

Item Number

G413546

Grouped product items
SKU	Size	Availability	Price
G413546-5mg	5mg	In stock	$93.90
G413546-10mg	10mg	In stock	$142.90
G413546-25mg	25mg	In stock	$266.90
G413546-50mg	50mg	In stock	$399.90
G413546-100mg	100mg	In stock	$602.90

ROR Agonists

View related series

RAR-related orphan receptor-γ Agonist

Basic Description

Synonyms	GSK2981278\|1474110-21-8\|ROR gama modulator 1\|N-(4-ethylphenyl)-3-(hydroxymethyl)-N-isobutyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)benzenesulfonamide\|GSK-2981278\|CHEMBL4225088\|L49V5G013I\|N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-(oxan-4-ylmet
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	GSK2981278 is a highly potent and selective inverse agonist for RORγ.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	AGONIST
Mechanism of action	Agonist of RAR-related orphan receptor-γ
Product Description	Information GSK2981278 GSK2981278 is a highly potent and selective inverse agonist for RORγ . Targets RORγ In vitro GSK2981278 has no significant effect on RORα-dependent activation. GSK2981278 significantly inhibits production of the Th17 signature (IL-17A, IL-17F, IL-22 and IL-23) in multiple in vitro and human tissue-based assays. In vivo GSK2981278 attenuates inflammation in a mouse model of psoriasis. Topical treatment with GSK2981278 will significantly limit Th17-type cytokine expression and should therefore lead to improved clinical outcomes for patients.

Product Properties

ALogP	4.456
HBD Count	1
Rotatable Bond	10

Associated Targets

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RORC Tchem Nuclear receptor ROR-gamma 4 Activities

Discover Target: RORC

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Discover Target: CSNK1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Discover Target: TRIM24

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Discover Target: BRPF1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzenesulfonamide
INCHI	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
InChi Key	LZLBRISQTJVZNP-UHFFFAOYSA-N
Canonical SMILES	CCC1=CC=C(C=C1)N(CC(C)C)S(=O)(=O)C2=CC(=C(C=C2)OCC3CCOCC3)CO
Isomeric SMILES	CCC1=CC=C(C=C1)N(CC(C)C)S(=O)(=O)C2=CC(=C(C=C2)OCC3CCOCC3)CO
PubChem CID	89875987
Molecular Weight	461.61

Database links

PubChem CID	89875987
CAS Registry No.	1474110-21-8

Certificates

Certificate of Analysis(COA)

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5 results found

Lot Number	Certificate Type	Date	Item
G2227601	Certificate of Analysis	Jun 12, 2022	G413546
G2227602	Certificate of Analysis	Jun 12, 2022	G413546
G2227603	Certificate of Analysis	Jun 12, 2022	G413546
G2227835	Certificate of Analysis	Jun 12, 2022	G413546
G2227838	Certificate of Analysis	Jun 12, 2022	G413546

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 92 mg/mL (199.3 mM); Ethanol: 92 mg/mL (199.3 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	92
DMSO(mM) Max Solubility	199.302441454908
Water(mg / mL) Max Solubility	＜1

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection.

References

1. Skepner J, Ramesh R, Trocha M, Schmidt D, Baloglu E, Lobera M, Carlson T, Hill J, Orband-Miller LA, Barnes A et al.. (2014) Pharmacologic inhibition of RORγt regulates Th17 signature gene expression and suppresses cutaneous inflammation in vivo.. J Immunol, 192 (6): (2564-75). [PMID:24516202]
2. Smith SH, Peredo CE, Takeda Y, Bui T, Neil J, Rickard D, Millerman E, Therrien JP, Nicodeme E, Brusq JM et al.. (2016) Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin.. PLoS ONE, 11 (2): (e0147979). [PMID:26870941]

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