Cutamesine dihydrochloride

SKU: orb1223248

Description

Cutamesine dihydrochloride is a selective σ1 receptor agonist (IC50: 17.4 nM). It shows selectivity for σ1 over σ2 receptors, and inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. In a rat model of experimental stroke, it enhances brain plasticity and sensorimotor function.(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. 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. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1.(In Vivo):Cutamesine extends the survival time in the SOD1G93A mice.

Key Properties

• CAS Number: 165377-44-6
• MW: 441.43
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₂N₂O₂·2HCl
• SMILES: COc1c(cc(cc1)CCN1CCN(CC1)CCCc1ccccc1)OC.Cl.Cl
• Target: GluR
• Solubility: DMSO : 30 mg/mL 67.96 mM

Bioactivity

• In Vivo:
  Cutamesine extends the survival time in the SOD1G93A mice.
• 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. 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. Cutamesine reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SA4503 (dihydrochloride) | AGY94806 dihydrochloride

Quick Database Links

Gene Symbol

GluR