SR1078

SKU: orb1302726

Description

SR1078 is a synthetic small molecule agonist that selectively activates the nuclear receptors RORα and RORγ. It is a valuable research tool for studying Th17 cell differentiation, cytokine production, and the role of these receptors in autoimmune and inflammatory diseases, as demonstrated in both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1246525-60-9
• MW: 431.25
• Purity: 99.58%
• Formula: C₁₇H₁₀F₉NO₂
• SMILES: OC(c1ccc(NC(=O)c2ccc(cc2)C(F)(F)F)cc1)(C(F)(F)F)C(F)(F)F
• Target: ROR
• Solubility: DMSO:45 mg/mL (104.35 mM)

Bioactivity

• In Vivo:
  The pharmacokinetics of SR1078 were evaluated in mice, revealing notable exposure. Plasma concentration 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.
• In Vitro:
  SR1078 is a synthetic RORα/RORγ li and that modulate the conformation of RORγ in biochemical assays and activates RORα and RORγ-driven transcription. It stimulate 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 li and-binding domain cotransfection assay, SR1078 significantly inhibit 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 activit.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

SR 1078, SR1078, SR-1078, ROR, RORα, RORγ, RAR-related orphan receptor, Inhibitor, inhibit

Compound Identifiers

PubChem CID

17980288