| Name | SR1078 |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (104.35 mM)
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| Keywords | inhibit | SR1078 | SR-1078 | ROR | RAR-related orphan receptor | Inhibitor |
| Inhibitors Related | S18-000003 | T0901317 | GSK2981278 | Nobiletin | XY101 | Cholesterol | AZD-0284 | Melatonin | SR2211 | Cabozantinib hydrochloride | RORγt Inverse agonist 6 | ML 209 |
| Related Compound Libraries | Nuclear Receptor Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Kinase Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Lipid Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
