5.33869
Sigma-2 Receptor Antagonist, CT01344
Synonym(s):
Sigma-2 Receptor Antagonist, CT01344, (R)-4-(3,4-dichlorophenyl)-N-(4-(trifluoromethyl)benzyl)butan-2-amine, PGRMC-1 Receptor Antagonist, CT01344
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All Photos(2)
About This Item
Empirical Formula (Hill Notation):
C18H18Cl2F3N
CAS Number:
Molecular Weight:
376.24
UNSPSC Code:
12352200
Recommended Products
assay
≥98% (HPLC)
Quality Level
form
oil
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
DMSO: 50 mg/mL
storage temp.
−20°C
General description
A cell-permeable, benzyl amine compound that can cross the blood-brain barrier and act as a selective antagonist of Sigma-2/progesterone receptor membrane component 1 (PGRMC1) receptor. Shown to competitively displace selective radioligand (3H-DTG) from homogenates of human B cell lines (Ki = 48 nM). Effectively blocks the effects of Abeta on membrane trafficking (EC50 = 8.7 µM) and displaces Abeta binding on cultured neurons (EC50 = 3.9 µM). It can also reverse Abeta oligomer-mediated trafficking deficits (EC50 = 7.3 µM) and restore normal synaptic function and cognitive abilities in a murine model of Alzheimer′s disease (10 - 30 mg/kg. p.o. over a period of 5.5 months). Shown to be effective when added either 1 hour prior to or 1 hour after Abeta oligomer preparations.
A cell-permeable, benzyl amine compound that can cross the blood-brain barrier and act as a selective antagonist of Sigma-2/progesterone receptor membrane component 1 (PGRMC1) receptor. Shown to competitively displace selective radioligand (3H-DTG) from homogenates of human B cell lines (Ki = 48 nM). Effectively blocks the effects of Abeta on membrane trafficking (EC50 = 8.7 µM) and displaces Abeta binding on cultured neurons (EC50 = 3.9 µM). It can also reverse Abeta oligomer-mediated trafficking deficits (EC50 = 7.3 µM) and restore normal synaptic function and cognitive abilities in a murine model of Alzheimer′s disease (10 - 30 mg/kg. p.o. over a period of 5.5 months). Shown to be effective when added either 1 hour prior to or 1 hour after Abeta oligomer preparations.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Primary Target
Sigma-2
Sigma-2
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Izzo, P.M., et al. 2014. Plos One.9, e111898.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
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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