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508578
Sigma-AldrichTSPO Agonist, Ro5-4864 - CAS 14439-61-3 - Calbiochem
A 4'-chloro derivative of diazepam that lacks affinity for GABA-A receptors, but can serve as a ligand for the peripheral benzodiazepine receptor.
More>>A 4'-chloro derivative of diazepam that lacks affinity for GABA-A receptors, but can serve as a ligand for the peripheral benzodiazepine receptor. Less<<
MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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.
Catalogue Number
508578
Brand Family
Calbiochem®
Synonyms
4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864
References
References
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.
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
18-April-2014 JSW
Synonyms
4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864
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.
Form
Off-white powder
Intert gas (Yes/No)
Packaged under inert gas
CAS number
14439-61-3
Chemical formula
C₁₆H₁₂Cl₂N₂O
Purity
≥98% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
Protect from light +2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
