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SR1078 is a newly described synthetic RORα/γ agonist. Treatment of cancer cells with SR1078 leads to p53 stabilization and induction of apoptosis. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. Furthermore, SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. Pharmacokinetic studies indicate that SR1078 displays reasonable exposure following injection into mice, and consistent with SR1078 functioning as a RORα/RORγ agonist, expression of two ROR target genes, glucose-6-phosphatase and fibroblast growth factor 21, were stimulated in the liver. Thus, SR1078 can be utilized as a chemical tool to probe the function of these receptors both in vitro and in vivo.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 cells |
| Preparation method | 16 h post-transfection, the cells were treated with vehicle or compound. 24 h post-treatment, the luciferase activity was measured using the Dual-GloTM luciferase assay system. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | C57BL6 mice |
| Formulation | |
| Dosages | 10 mg/kg |
| Administration | i.p. |
| Molecular Weight | 431.25 |
| Formula | C17H10F9NO2 |
| CAS Number | 1246525-60-9 |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ROR Products |
|---|
| Dehydrolithocholic acid
Dehydrolithocholic acid is a bile acid metabolite, which inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM). |
| SR3335
SR3335 (ML-176) is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. |
| SR 1001
SR 1001 is a RORα/γ inverse agonist with Ki values of 172 and 111 nM, respectively. |
| GSK2981278
GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). |
| SR2211
SR2211 is a synthetic RORγ-selective modulator, functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM. |
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