SR1001

Names

[ Name ]:
SR1001

[Synonym ]:
5-(methylsulfonamido)pyridin-3-ylboronic acid pinacol ester
N-(5-(N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)sulphamoyl)-4-methylthiazol-2-yl)acetamide
Acetamide, N-[4-methyl-5-[[[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]amino]sulfonyl]-2-thiazolyl]-
N-(5-{[4-(1,1,1,3,3,3-Hexafluoro-2-hydroxy-2-propanyl)phenyl]sulfamoyl}-4-methyl-1,3-thiazol-2-yl)acetamide
N-[5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl]methansulphonamide
N-(5-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)methanesulfonamide
N-(5-(cyclopropylcarbamoyl)-2-methylphenyl)-5-methyl-1-(3-(trifluoromethyl)pyridin-2-yl)-1H-pyrazole-4-carboxamide
SR1001

Biological Activity

[Description]:

SR1001 is a selective RORα and RORγ inverse agonist; inhibits TH17 cell differentiation and function.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> ROR

Research Areas >> Inflammation/Immunology

[In Vitro]

SR1001 inhibits the development of murine TH17 cells by inhibition of IL-17A gene expression and protein production. SR1001 reduces the interaction of a coactivator TRAP220 NR box 2 peptide with RORγ in a dose dependent manner (IC50 value≈117 nM). Additionally, SR1001 inhibits the expression of cytokines when added to differentiated murine or human TH17 cells[1].

[In Vivo]

SR1001 effectively suppresses the clinical severity of autoimmune disease in mice. Administration of SR1001 to C57BL/6 mice suppresses the expression of hepatic ROR target genes, Cyp7b1, Rev-erbα, and Serpine 1[1]. SR1001 a RORα inverse agonist eliminats the circadian pattern of expression of citrate synthase mRNA in mice[2].

[Cell Assay]

HEK293 cells are plated in 96-well plates at a density of 15 x 103 cells/well. Transfections are performed using Lipofectamine 2000. 24 h post-transfection, the cells are treated with vehicle or compound (SR1001). 24 h post-treatment, the luciferase activity is measured using the Dual-Glo luciferase assay system[1].

[Animal admin]

Mice: Experimental autoimmune encephalomyelitis is induced in C57BL/6 wild-type mice by s.c. injection over four sites in the flank with 200 μg per mouse. The SR1001 is dissolved in DMSO at 25 mg/mL and the mice are treated (i.p.) with 25 mg/kg SR1001 (1 μL/g body weight of mouse) or vehicle (DMSO, 1 μL/g body weight of mouse) twice per day. The treatment is started 2 days before immunization and continued until the end of experiment[1].

[References]

[1]. Solt LA, et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. Nature. 2011 Apr 28;472(7344):491-4.

[2]. Crumbley C, et al. Regulation of expression of citrate synthase by the retinoic acid receptor-related orphan receptor α (RORα). PLoS One. 2012;7(4):e33804.

[Related Small Molecules]

SR1078 | LYC-55716 | SR3335 | ROR gamma-t-IN-1 | GSK2981278 | SR2211 | Gne-0946 | GNE-6468 | L 601920-0 | RORγ-IN-1 | SR 0987 | TMP778

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C₁₅H₁₃F₆N₃O₄S₂

[ Molecular Weight ]:
477.402

[ Exact Mass ]:
477.025177

[ PSA ]:
148.50000

[ LogP ]:
3.15

[ Index of Refraction ]:
1.557

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H319

[ Precautionary Statements ]:
P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport

Precursor & DownStream

Precursor

DownStream

Articles

JAK/STAT regulation of Aspergillus fumigatus corneal infections and IL-6/23-stimulated neutrophil, IL-17, elastase, and MMP9 activity.

J. Leukoc. Biol. 100 , 213-22, (2016)

IL-6 and IL-23 (IL-6/23) induce IL-17A (IL-17) production by a subpopulation of murine and human neutrophils, resulting in autocrine IL-17 activation, enhanced production of reactive oxygen species, a...

Related Compounds

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