5.31084
R55
≥92% (HPLC), powder, retromer chaperone, Calbiochem®
Synonym(s):
Retromer Chaperone, R55, Thiophene-2,5-diylbis(methylene) dicarbamimidothioate, HCl, Retromer Pharmacological Chaperone, R55
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About This Item
Empirical Formula (Hill Notation):
C8H12N4S3 · xHCl
CAS Number:
Molecular Weight:
260.40 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥92% (HPLC)
Form:
powder
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Product Name
Retromer Chaperone, R55,
assay
≥92% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
off-white
solubility
water: 50 mg/mL
storage temp.
2-8°C
SMILES string
[s]1c(ccc1CSC(=[N+H2])N)CSC(=[N+H2])N.[Cl-].[Cl-]
InChI key
DSODRWWHAUGSGD-UHFFFAOYSA-N
General description
A 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.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
vacuolar protein sorting (Vps) proteins
vacuolar protein sorting (Vps) proteins
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Mecozzi, V.J., et al. 2014. Nat. Chem. Biol.10, 443.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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