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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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Size/SKUAvailabilityPrice
25 mg
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$264.00

About This Item

Empirical Formula (Hill Notation):
C8H12N4S3 · xHCl
CAS Number:
2076-91-7
Molecular Weight:
260.40 (free base basis)
MDL number:
MFCD25976641
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥92% (HPLC)
Form:
powder
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

$264.00

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Product Name

Retromer Chaperone, R55,

assay

≥92% (HPLC)

Quality Segment

100

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
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)

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Retromer Chaperone, R55

Sigma-Aldrich

531084

Retromer Chaperone, R55

TSPO Agonist, Ro5-4864

Sigma-Aldrich

508578

TSPO Agonist, Ro5-4864

RAGE Antagonist, FPS-ZM1 RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (Ki = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE).

Sigma-Aldrich

553030

RAGE Antagonist, FPS-ZM1

γ-Secretase Inhibitor XXIII, Aβ42-Selective The γ-Secretase Inhibitor XXIII, Aβ42-Selective controls the biological activity of γ-Secretase.

Sigma-Aldrich

565792M

γ-Secretase Inhibitor XXIII, Aβ42-Selective

description

-

description

-

description

RAGE Antagonist, FPS-ZM1, is a blood-brain-barrier permeant blocker of RAGE V domain-mediated ligand binding (Ki = 25, 148, & 230 nM, respectively, against Aβ40, HMGB1 & S100B, binding to sRAGE).

description

The γ-Secretase Inhibitor XXIII, Aβ42-Selective controls the biological activity of γ-Secretase.

assay

≥92% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

form

powder

form

powder

form

semisolid, viscous liquid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light, desiccated (hygroscopic)

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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