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

508578
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₆H₁₂Cl₂N₂O 14439-61-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08578.0001
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          Glass bottle 10 mg
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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
          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

          Documentation

          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 +2°C to +8°C
          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.
          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.