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SR3335 suppresses the expression of endogenous RORα target genes in HepG2 involved in hepatic gluconeogenesis including glucose-6-phosphatase and phosphoenolpyruvate carboxykinase. The first selective synthetic RORα inverse agonists may hold utility for suppression of elevated hepatic glucose production in type 2 diabetics.
| 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 | |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | 30 week old Diet induced obese (DIO) C57BL/6 male mice |
| Formulation | 65% Kcal high-fat diet |
| Dosages | 15 mg/kg |
| Administration | i.p. |
| Molecular Weight | 405.34 |
| Formula | C13H9F6NO3S2 |
| CAS Number | 293753-05-6 |
| 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). |
| SR1078
SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ; increases transcription of RORα target genes; thought to increase p53 stability. |
| 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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