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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

Products

Catalogue NumberPackaging Qty/Pack
5310840001 Glass bottle 25 mg
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
5310840001 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.