Cutamesine 2HCl

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Chemical Structure| 165377-44-6 同义名 : 库他美新二盐酸盐 ;SA4503 dihydrochloride; AGY94806 dihydrochloride; Cutamesine; AGY 94806; SA 4503; Cutamesine dihydrochloride
CAS号 : 165377-44-6
货号 : A260566
分子式 : C23H34Cl2N2O2
纯度 : 99%+
分子量 : 441.43
MDL号 : MFCD00939308
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(67.96 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(226.53 mM)，配合低频超声助溶
生物活性
描述 SA4503 dihydrochloride is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. SA4503 is 14-fold selective for sigma(1) (K(i) = 4.6 nM) over sigma(2) (K(i) = 63.1 nM) sites in guinea pig brain homogenates[3]. SA4503 blocks neuronal cell death via repressing activation of the MAPK/ERK (mitogen-activated protein kinase/extracellular signal-regulated kinase) pathway and, consequently, expression levels of glutamate receptors[4]. SA4503 (0.3-1.0mg/kg) administration rescued PO (pressure overload)-induced σ1R decreases in aortic smooth muscle and endothelial cells. SA4503 treatment also rescued PO-induced impairments in ACh- and clonidine-induced vasodilation without affecting PE- and ET-1-induced vasoconstriction[5]. Significant decreases in the BDNF(brain-derived neurotrophic factor)-protein level in the medial prefrontal cortex of ATR-X (α-thalassemia X-linked intellectual disability) model mice were recovered with treatment of SA4503[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.27mL

0.45mL

0.23mL

11.33mL

2.27mL

1.13mL

22.65mL

4.53mL

2.27mL
参考文献

[1]Shimazawa M, Sugitani S, et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage. Exp Eye Res. 2015 Mar;132:64-72.

[2]Matsuno K, Nakazawa M, et al. Binding properties of SA4503, a novel and selective sigma 1 receptor agonist. Eur J Pharmacol. 1996 Jun 13;306(1-3):271-9.

[3]Lever JR, Gustafson JL, Xu R, Allmon RL, Lever SZ. Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8

[4]Tuerxun T, Numakawa T, Adachi N, Kumamaru E, Kitazawa H, Kudo M, Kunugi H. SA4503, a sigma-1 receptor agonist, prevents cultured cortical neurons from oxidative stress-induced cell death via suppression of MAPK pathway activation and glutamate receptor expression. Neurosci Lett. 2010 Jan 29;469(3):303-8

[5]Tagashira H, Matsumoto T, Taguchi K, Zhang C, Han F, Ishida K, Nemoto S, Kobayashi T, Fukunaga K. Vascular endothelial σ1-receptor stimulation with SA4503 rescues aortic relaxation via Akt/eNOS signaling in ovariectomized rats with aortic banding. Circ J. 2013;77(11):2831-40

[6]Yamaguchi K, Shioda N, Yabuki Y, Zhang C, Han F, Fukunaga K. SA4503, A Potent Sigma-1 Receptor Ligand, Ameliorates Synaptic Abnormalities and Cognitive Dysfunction in a Mouse Model of ATR-X Syndrome. Int J Mol Sci. 2018 Sep 18;19(9):2811