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508578 TSPO Agonist, Ro5-4864 - CAS 14439-61-3 - Calbiochem

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CAS #Empirical Formula
14439-61-3C₁₆H₁₂Cl₂N₂O

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5.08578.0001
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      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
      Biological Information
      Primary TargetTSPO
      Primary Target K<sub>i</sub>4.4 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Référence GTIN
      5.08578.0001 04055977262070