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531084 Retromer Chaperone, R55 - CAS 2076-91-7 - Calbiochem

A cell-permeable pharmacological chaperone to increase neuronal retromer levels. Improves Vps35-Vps29-Vps26 retromer complex stability.

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

Synonyms: Thiophene-2,5-diylbis(methylene) dicarbamimidothioate, HCl, Retromer Pharmacological Chaperone, R55

Primary Target: vacuolar protein sorting (Vps) proteins
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531084
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
2076-91-7C₈H₁₂N₄S₃ • HCl

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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
      CAS number2076-91-7
      FormOff-white powder
      Hill FormulaC₈H₁₂N₄S₃ • HCl
      Chemical formulaC₈H₁₂N₄S₃ • HCl
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.31084.0001 04055977242584

      Documentation

      Retromer Chaperone, R55 - CAS 2076-91-7 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Retromer Chaperone, R55 - CAS 2076-91-7 - Calbiochem Certificates of Analysis

      TitleLot Number
      531084

      References

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

      Brochure

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

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage.
      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
      CAS number2076-91-7
      Chemical formulaC₈H₁₂N₄S₃ • HCl
      Purity≥92% by HPLC
      SolubilityH₂O (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesMecozzi, V.J., et al. 2014. Nat. Chem. Biol. 10, 443.