SR2211

Names

[ Name ]:
SR2211

[Synonym ]:
1,1,1,3,3,3-Hexafluoro-2-(2-fluoro-4'-{[4-(4-pyridinylmethyl)-1-piperazinyl]methyl}-4-biphenylyl)-2-propanol
[1,1'-Biphenyl]-4-methanol, 2-fluoro-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-

Biological Activity

[Description]:

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> ROR

Research Areas >> Inflammation/Immunology

[Target]

IC50: ~320 nM (RORγ), Ki: 105 nM (RORγ)[1][2].

[In Vitro]

The treatment of EL4 with SR2211 represses the Il17 gene expression to a greater extent as compared to digoxin. Similarly, the expression of IL-23 receptor (Il23r) is significantly inhibited by SR2211 and digoxin, as has been previously reported. Treatment of EL-4 cells with SR2211 as well as a control digoxin results in significant inhibition of IL-17 intracellular staining as compared to vehicle treated cells[1].

[References]

[1]. Kumar N, et al. Identification of SR2211: a potent synthetic RORγ-selective modulator. ACS Chem Biol. 2012 Apr 20;7(4):672-7.

[2]. Song Y, et al. Identification of N-phenyl-2-(N-phenylphenylsulfonamido)acetamides as new RORγ inverse agonists: Virtual screening, structure-based optimization, and biological evaluation. Eur J Med Chem. 2016 Jun 30;116:13-26.

[Related Small Molecules]

SR1078 | LYC-55716 | SR3335 | ROR gamma-t-IN-1 | SR1001 | GSK2981278 | Gne-0946 | GNE-6468 | L 601920-0 | RORγ-IN-1 | SR 0987 | TMP778

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
552.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₆H₂₄F₇N₃O

[ Molecular Weight ]:
527.477

[ Flash Point ]:
287.9±30.1 °C

[ Exact Mass ]:
527.180786

[ PSA ]:
39.60000

[ LogP ]:
4.79

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.545

[ Storage condition ]:
2-8℃

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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