General description
A selective, cell-permeable ligand (EC50 = 250 nM) that acts as a REV-ERBα agonist using a FRET assay. It enhances the recruitment of NCoR peptide to REV-ERBα by up to 70%, and displays no activity towards LRH1, SF1, FXR or ROR, and LXR. Furthermore, it inhibits the promoter activity of Pai1, a known target for REV-ERBα by 30%. This ligand exhibits acute suppression of Bmal1 transcription, and is capable of resetting the molecular rhythm of REV-ERBα-mediated PER2 expression in both Rat-1 lung fibroblasts and on ectopic lung tissues in Luciferase reporter assays. In addition, it is shown to repress the expression of gluconeogenic genes in liver cells and reduce glucose output in primary hepatocytes.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Grant, D., et al. 2010, ACS Chem. Biol.5, 925.
Meng, Q., et al. 2008. Journ. Cell. Sci121, 3629.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 396.89. Empirical Formula: C18H21ClN2O4S. Quality Level: 100. Assay: ≥. 95% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: dark beige. solubility: DMSO: 50 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.Shipping Information:
Dry Ice Surcharge & Ice Pack Shipments: $40
More Information: https://cenmed.com/shipping-returns
- UPC:
- 12352200
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 554716-10MG
- Temperature Control Device:
- Yes
