Cutamesine dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cutamesine diHClide 是一种选择性 σ1 受体激动剂 (IC50: 17.4 nM)。

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.

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.

Cutamesine extends the survival time in the SOD1G93A mice.

SA4503 (dihydrochloride) | AGY94806 dihydrochloride

Neuroscience

GluR

σ1

Neurological Disease

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165377-44-6

441.43

C23H32N2O2·2HCl

>98% (HPLC)

DMSO : 30 mg/mL 67.96 mM;

COc1c(cc(cc1)CCN1CCN(CC1)CCCc1ccccc1)OC.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years