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SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $35 | In Stock | In Stock | |
| 2 mg | $50 | In Stock | In Stock | |
| 5 mg | $82 | In Stock | In Stock | |
| 10 mg | $117 | In Stock | In Stock | |
| 25 mg | $238 | In Stock | In Stock | |
| 50 mg | $387 | In Stock | In Stock | |
| 100 mg | $575 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $84 | In Stock | In Stock |
| Description | SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ. |
| In vitro | SR1078 is a synthetic RORα/RORγ ligand that modulates the conformation of RORγ in biochemical assays and activates RORα and RORγ-driven transcription. It stimulates the expression of endogenous ROR target genes in HepG2 cells expressing both RORα and RORγ. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand-binding domain cotransfection assay, SR1078 significantly inhibits the constitutive transactivation activity of RORα and RORγ, without affecting FXR, LXRα, or LXRβ. Treatment of cells with SR1078 (10 μM) in a RORα cotransfection assay significantly increases transcription, and similarly, in a RORγ cotransfection assay, SR1078 stimulates RORγ-dependent transcription activity[1]. |
| In vivo | The pharmacokinetics of SR1078 were evaluated in mice, revealing notable exposure. Plasma concentrations reached 3.6 μM one hour post 10 mg/kg i.p. injection and remained above 800 nM at 8 hours. These levels are adequate for proof-of-principle experiments assessing ROR target gene expression. Mice treated with SR1078 (10 mg/kg i.p.) showed significant stimulation of both G6Pase and FGF21 gene expression in liver mRNA, compared to vehicle control [1]. |
| Synonyms | SR 1078 |
| Molecular Weight | 431.25 |
| Formula | C17H10F9NO2 |
| Cas No. | 1246525-60-9 |
| Smiles | OC(c1ccc(NC(=O)c2ccc(cc2)C(F)(F)F)cc1)(C(F)(F)F)C(F)(F)F |
| Relative Density. | 1.527 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (104.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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