Selective inverse agonist of RORγ
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SR 2211

Item No. 11972

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-fluoro-4’-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1’-biphenyl]-4-methanol
CAS Number
1359164-11-6
Molecular Formula
C26H24F7N3O
Formula Weight
527.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/ml
λmax
251 nm
SMILES
OC(C(F)(F)F)(C1=CC(F)=C(C2=CC=C(CN3CCN(CC4=CC=NC=C4)CC3)C=C2)C=C1)C(F)(F)F
InChi Code
InChI=1S/C26H24F7N3O/c27-23-15-21(24(37,25(28,29)30)26(31,32)33)5-6-22(23)20-3-1-18(2-4-20)16-35-11-13-36(14-12-35)17-19-7-9-34-10-8-19/h1-10,15,37H,11-14,16-17H2
InChi Key
KVHKWAZUPPBMLL-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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    1 mg

    $41

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    5 mg

    $148

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    10 mg

    $178

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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 differentiation of pro-inflammatory TH17 cells, which are implicated in autoimmune diseases like multiple sclerosis and rheumatoid arthritis.1,2 SR 2211 selectively binds RORγ (Ki = 105 nM), acting as an inverse agonist of constitutive in vitro RORγ activity (IC50 = 320 nM).3 It has minimal effects on RORα, LXRα, and FXR activities. SR 2211 significantly inhibits gene expression of IL-17 and IL-23 receptor in activated EL-4 mouse T lymphocytes when given at 5 μM.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 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. Kumar, N., Lyda, B., Chang, M.R., et al. Identification of SR2211: A potent synthetic RORγ-selective modulator. ACS Chem. Biol. 7(4), 672-677 (2012).