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508578 TSPO 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864

Primary Target: TSPO
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
14439-61-3C₁₆H₁₂Cl₂N₂O

Products

Catalog NumberPackaging Qty/Pack
5.08578.0001 Glass bottle 10 mg
Description
OverviewA 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 Number508578
Brand Family Calbiochem®
Synonyms4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864
References
ReferencesBarron, 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.
Product Information
CAS number14439-61-3
FormOff-white powder
Hill FormulaC₁₆H₁₂Cl₂N₂O
Chemical formulaC₁₆H₁₂Cl₂N₂O
Quality LevelMQ100
Applications
Biological Information
Primary TargetTSPO
Primary Target K<sub>i</sub>4.4 nM
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.08578.0001 04055977262070

Documentation

TSPO Agonist, Ro5-4864 - CAS 14439-61-3 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
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.

Revision18-April-2014 JSW
Synonyms4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864
DescriptionA 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.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number14439-61-3
Chemical formulaC₁₆H₁₂Cl₂N₂O
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesBarron, 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.