1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
  3. Cutamesine dihydrochloride

Cutamesine dihydrochloride (Synonyms: SA4503 dihydrochloride; AGY94806 dihydrochloride)

Cat. No.: HY-13510 Purity: 99.48%
Handling Instructions

Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.

For research use only. We do not sell to patients.

Cutamesine dihydrochloride Chemical Structure

Cutamesine dihydrochloride Chemical Structure

CAS No. : 165377-44-6

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10 mM * 1 mL in DMSO USD 157 In-stock
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10 mg USD 143 In-stock
Estimated Time of Arrival: December 31
50 mg USD 604 In-stock
Estimated Time of Arrival: December 31
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Description

Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.

IC50 & Target

IC50: 17.4 nM (σ1receptor, guinea pig brain membranes)[1]

In Vitro

The sigma receptor might be involved in several diseases in the central nervous system. Cutamesine, a potent σ1receptor agonist, has 103-fold higher affinity for σ1 (IC50=17.4 nM) than σ2 (IC50=1,784 nM) sites in guinea pig brain membranes. Cutamesine is 14-fold selective for σ1 (Ki=4.6 nM) over σ2 (Ki=63.1 nM) sites in guinea pig brain homogenates[1]. Cutamesine protects motor neuron NSC34 cells against superoxide dismutase 1 and serum free neurotoxicity. It upregulates the phosphorylation levels of Akt and extracellular signal-regulated kinase (ERK) 1/2[2]. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cutamesine extends the survival time in the SOD1G93A mice[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

441.43

Formula

C₂₃H₃₄Cl₂N₂O₂

CAS No.
SMILES

COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (67.96 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2654 mL 11.3268 mL 22.6536 mL
5 mM 0.4531 mL 2.2654 mL 4.5307 mL
10 mM 0.2265 mL 1.1327 mL 2.2654 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.27 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

The NSC34 cells are seeded at a density of 7000 cells per well into 96-well plates with D-MEM and transfected using Lipofectamine 2000 mixed with 2 μg /mL of plasmid vector in D-MEM for 6 h. After 6 h, the cell-culture medium is replaced with fresh D-MEM and culture and allowed to proceed for a further 42 h. The cells are then transferred to serum-free D-MEM and immediately treated with Cutamesine at a final concentration of 1, 3, or 10 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Transgenic female mice overexpressing mutated human SOD1G93A are used in the study. Cutamesine is dissolved in saline and subcutaneously administered at a dose of 1 mg/kg once daily to 5-week-old SOD1G93A mice to the time of death. In a control group, vehicle (saline) is subcutaneously administered at 10 ml/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CutamesineSA4503AGY94806SA 4503SA-4503AGY 94806AGY-94806Sigma ReceptorInhibitorinhibitorinhibit

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Product Name:
Cutamesine dihydrochloride
Cat. No.:
HY-13510
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