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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.

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

Primary Target: TSPO
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508578
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
14439-61-3C₁₆H₁₂Cl₂N₂O

Preis & Verfügbarkeit

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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
      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
      Bestellnummer GTIN
      5.08578.0001 04055977262070

      Documentation

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

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      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.
      Datenblatt

      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.