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Merck

5.31084

R55

≥92% (HPLC), powder, retromer chaperone, Calbiochem®

別名:

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

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この商品について

実験式(ヒル表記法):
C8H12N4S3 · xHCl
CAS番号:
分子量:
260.40 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥92% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze
desiccated (hygroscopic)
protect from light
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製品名

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

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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グローバルトレードアイテム番号

カタログ番号GTIN
5.31084.000104055977242584

ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.

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