A modulator of RORγ and LXR receptors
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SR 1903

Item No. 28253

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2'-methyl-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-α,α-bis(trifluoromethyl)-[1,1'-biphenyl]-4-methanol
CAS Number
1414248-06-8
Molecular Formula
C27H27F6N3O
Formula Weight
523.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/ml
λmax
249 nm
SMILES
CC1=C(C2=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C2)C=CC(CN(CC3)CCN3CC4=CC=NC=C4)=C1
InChi Code
InChI=1S/C27H27F6N3O/c1-19-16-21(18-36-14-12-35(13-15-36)17-20-8-10-34-11-9-20)2-7-24(19)22-3-5-23(6-4-22)25(37,26(28,29)30)27(31,32)33/h2-11,16,37H,12-15,17-18H2,1H3
InChi Key
HSUQYJQLSYQEOB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chang, M.R., Ciesla, A., Strutzenberg, T.S., et al. Unique polypharmacology nuclear receptor modulator blocks inflammatory signaling pathways. ACS Chem. Biol. 14(5), 1051-1062 (2019).