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
• Empirical Formula (Hill Notation): C₁₈H₁₈Cl₂F₃N
• CAS Number: 1425092-22-3
• Molecular Weight: 376.24
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• 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

Description

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 (K_i = 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 (K_i = 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.

Biochem/physiol Actions

Primary Target
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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable