| Identification | Back Directory | [Name]
Ethanone, 1-[4-[[4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]methyl]-1-piperazinyl]-, hydrochloride (1:1) | [CAS]
2309312-90-9 | [Synonyms]
Ethanone, 1-[4-[[4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]methyl]-1-piperazinyl]-, hydrochloride (1:1) | [Molecular Formula]
C22H23ClF6N2O2 | [MOL File]
2309312-90-9.mol | [Molecular Weight]
496.88 |
| Hazard Information | Back Directory | [Description]
Retinoic acid receptor-related nuclear receptor γ (RORγ) plays a central role in T cell differentiation, particularly in the development of TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.1,2 SR 1555 is a selective ligand of RORγ (IC50 = 1 μM).3 It does not bind RORα, LXR, or FXR. SR 1555 acts as an inverse agonist of RORγ, inhibiting endogenous IL-17A gene expression in mouse splenocytes and suppressing differentiation of TH17 cells when cultured under TH17 polarizing conditions.3 Moreover, SR 1555 stimulates T regulatory development when cultured under T regulatory polarizing conditions, unlike digoxin and ursolic acid.3 | [Uses]
SR1555 hydrochloride is the hydrochloride salt form of SR1555 (HY-120785). SR1555 hydrochloride is an inverse agonist for retinoic acid receptor-related orphan nuclear receptor γ (RORγ) with an IC50 of 1 μM. SR1555 hydrochloride inhibits the development and function of pro-inflammatory TH17 cell, increases the frequency of anti-inflammatory T regulatory (Treg) cells. SR1555 hydrochloride can be used for research about autoimmune diseases[1]. | [References]
1. Ivanov, I.I., McKenzie, B.S., Zhou, L., et al. The orphan nuclear receptor RORγt directs the differentiation program of proinflammatory IL-17+ T helper cells Cell 126(6),1121-1133(2006).
2. Solt, L.A., Kumar, N., Nuhant, P., et al. Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand Nature 472(7344),491-494(2011).
3. Solt, L.A., Kumar, N., He, Y., et al. Identification of a selective RORγ ligand that suppresses TH17 cells and stimulates T regulatory cells ACS Chem. Biol. 7,1515-1519(2012). |
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Biorbyt Ltd.
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