Stenabolic (SR9009) is an agonist of REV-ERB, with IC50 of 670 nM and 800 nM for REV-ERBα and REV-ERBβ respectively. Stenabolic (SR9009) inhibits the activity of the SCN clock, with reversible inhibition of circadian oscillations in SCN explants cultured from the Per2:luc reporter mouse. Stenabolic (SR9009) dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter. Stenabolic (SR9009) potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9009 IC50=710 nM).
Cell Experiment | |
---|---|
Cell lines | L929 cell |
Preparation method | Cells were treated with 100 ng/ml IFNg (Millipore) and 10 ng/ml LPS(Millipore) for M1 polarization. M2 differentiation was induced by incubating macrophages with 15 ng/ml IL-4 (Millipore). |
Concentrations | 10 μM |
Incubation time | 24 h |
Animal Experiment | |
---|---|
Animal models | homozygous LDL receptor deficient (ldlr−/−) male mice |
Formulation | PBS |
Dosages | 100 mg/kg |
Administration |
Molecular Weight | 437.94 |
Formula | C20H24ClN3O4S |
CAS Number | 1379686-30-2 |
Solubility (25°C) | DMSO ≥ 60 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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.