An inverse agonist of RORγ
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SR 1555 (hydrochloride)

Item No. 12071

Technical Information
Formal Name
1-[4-[[4'-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl][1,1'-biphenyl]-4-yl]methyl]-1-piperazinyl]-ethanone, monohydrochloride
CAS Number
2309312-90-9
Molecular Formula
C22H22F6N2O2 • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:6): 0.16 mg/mlDMSO: 3 mg/mlEthanol: 1.6 mg/ml
λmax
203, 257 nm
SMILES
O=C(C)N(CC1)CCN1CC2=CC=C(C3=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C3)C=C2.Cl
InChi Code
InChI=1S/C22H22F6N2O2.ClH/c1-15(31)30-12-10-29(11-13-30)14-16-2-4-17(5-3-16)18-6-8-19(9-7-18)20(32,21(23,24)25)22(26,27)28;/h2-9,32H,10-14H2,1H3;1H
InChi Key
OHUOFZJUUXXRGG-UHFFFAOYSA-N
License
Sold under license from The Scripps Research Institute.
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ivanov, I.I., McKenzie, B.S., Zhou, L., et alThe 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 alSuppression 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 alIdentification of a selective RORγ ligand that suppresses TH17 cells and stimulates T regulatory cells. ACS Chem. Biol. 7(9), 1515-1519 (2012).