531084 Retromer Chaperone, R55 - Calbiochem

531084
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₈H₁₂N₄S₃ • HCl

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.31084.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, non-toxic thienyl bis-isothiourea derived compound that acts as a pharmacological chaperone to increase neuronal retromer levels and improve the stability of trimeric Vps35-Vps29-Vps26 retromer complex. Shown to significantly increase the level of Vsp35 (EC50 = 3.3 µM) and Vsp29 in hippocampal neurons. Binds at the interface between Vps35 and Vps29 (Kd = 5 µM) and interacts with side chains from both proteins. However, it does not affect the thermal unfolding of individual proteins and has no effect on mRNA levels of Vps35 and Vsp29. Shown to reduce the endogenous levels of both Aβ40 and Aβ42 and is also effective in reducing human Aβ40 and -42 levels in J20 transgenic murine model of AD36 (IC50 ~ 12 µM). Also reduces the levels of both endogenous β-CTF and sAPPβ and increases the level of sAPPα in the medium. Displays a partial stabilizing effect on Vps35 even in the context of Vps29 knockdown.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531084
          Brand Family Calbiochem®
          SynonymsThiophene-2,5-diylbis(methylene) dicarbamimidothioate, HCl, Retromer Pharmacological Chaperone, R55
          References
          ReferencesMecozzi, V.J., et al. 2014. Nat. Chem. Biol. 10, 443.
          Product Information
          FormOff-white powder
          Hill FormulaC₈H₁₂N₄S₃ • HCl
          Chemical formulaC₈H₁₂N₄S₃ • HCl
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary Targetvacuolar protein sorting (Vps) proteins
          Purity≥92% 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 Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          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

          Retromer Chaperone, R55 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Mecozzi, V.J., et al. 2014. Nat. Chem. Biol. 10, 443.

          Brochure

          Title
          NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
          Neuroscience Solutions for productive research
          New Products - Antibodies, Small Molecule, Inhibitors

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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.

          Revision12-September-2014 JSW
          SynonymsThiophene-2,5-diylbis(methylene) dicarbamimidothioate, HCl, Retromer Pharmacological Chaperone, R55
          DescriptionA cell-permeable, non-toxic thienyl bis-isothiourea derived compound that acts as a pharmacological chaperone to increase neuronal retromer levels and improve the stability of trimeric Vps35-Vps29-Vps26 retromer complex. Shown to significantly increase the level of Vsp35 (EC50 = 3.3 µM) and Vsp29 in hippocampal neurons. Binds at the interface between Vps35 and Vps29 (Kd = 5 µM) and interacts with side chains from both proteins. However, it does not affect the thermal unfolding of individual proteins and has no effect on mRNA levels of Vps35 and Vsp29. Shown to reduce the endogenous levels of both Aβ40 and Aβ42 and is also effective in reducing human Aβ40 and -42 levels in J20 transgenic murine model of AD36 (IC50 ~ 12 µM). Also reduces the levels of both endogenous β-CTF and sAPPβ and increases the level of sAPPα in the medium. Displays a partial stabilizing effect on Vps35 even in the context of Vps29 knockdown.
          FormOff-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₈H₁₂N₄S₃ • HCl
          Purity≥92% by HPLC
          SolubilityH₂O (50 mg/ml)
          Storage +2°C to +8°C
          Hygroscopic
          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
          ReferencesMecozzi, V.J., et al. 2014. Nat. Chem. Biol. 10, 443.