Merck, 5085780001, TSPO Agonist, Ro5-4864

General description
A 4′-chloro derivative of diazepam that lacks affinity for GABA-A receptors, but can serve as a ligand for the peripheral benzodiazepine receptor. Acts as an agonist for the 18 kDa translocator protein (TSPO) on the outer mitochondrial membrane (Kd = 4.4 nM). Diminishes the accumulation of β-amyloid peptides in the CA1 hippocampal region of gonadectomized (GDX) mice and in triple transgenic Alzheimer′s disease murine models (3xTgAD). However, it does not affect tau phosphorylation events as assessed by AT8 immunoreactivity. Also shown to reduce GFAP ionized calcium binding adaptor molecule-1 (IBA-1) in the 3xTgAD mice. Reported to increase testosterone and progesterone levels in GDX mice without affecting other steroid hormones. However, it does not have a significant effect on the levels of these hormones in aged 3xTgAD mice. In combination with another mitochondria targeting molecule, lonidamine, it is shown to induce apoptosis in MDA-MB-231 breast cancer cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
TSPO
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Barron, A.M., et al. 2013. The J.Neuroscience.33, 8891.Yousefi, O.S., et al. 2013. Cell Commun.Signaling.11, 13.Wu, X., and Gallo, K.E. 2013. PLoS One.8, e71258.Leonelli, E., et al. 2005. Mech. Ageing. Dev.126, 1159.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)