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Merck

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
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Product Name

Retromer Chaperone, R55,

SMILES string

[s]1c(ccc1CSC(=[N+H2])N)CSC(=[N+H2])N.[Cl-].[Cl-]

InChI key

DSODRWWHAUGSGD-UHFFFAOYSA-N

assay

≥92% (HPLC)

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

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
vacuolar protein sorting (Vps) proteins
Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

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

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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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Global Trade Item Number

SKUGTIN
5.31084.000104055977242584

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