Treatment of HepG2 cells with SR8278 results in increased expression of REV-ERBα target genes consistent with the compound blocking the action of the endogenous agonist, heme. In a cell-based assay, SR8278 is considerably more potent than the other synthetic REV-ERBα ligand, GSK4112, which functions as an agonist. Like GSK4112, SR8278 displayed poor pharmacokinetic properties that will likely limit its use to biochemical and cell-based assays. SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 cells |
| Preparation method | Sixteen 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 | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 361.48 |
| Formula | C18H19NO3S2 |
| CAS Number | 1254944-66-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related REV-ERB Products |
|---|
| SR12418
SR12418 is a REV-ERB-specific synthetic ligand with IC50 values of 68 nM for REV-ERBα and 119 nM for REV-ERBβ. SR12418 can be used in studies related to experimental autoimmune encephalomyelitis (EAE) and colitis. |
| SR-29065
SR-29065 is a selective REV-ERBα agonist for autoimmune disease research. |
| STL1267
STL1267 is a potent REV-ERB agonist that crosses the blood-brain barrier with a Ki value of 0.16 µM for REV-ERBα. STL1267 showed no cytotoxicity and inhibited BMAL1 gene expression. |
| SR9011 hydrochloride
SR9011 hydrochloride is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
| SR9011
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
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