货号:A260566 同义名: 库他美新二盐酸盐 / SA4503 dihydrochloride;AGY94806 dihydrochloride
SA4503 2HCl is the 2HCl form of SA4503 which is an agonist of opioid sigma1 receptor (σ1R) with IC50 of 17.4 nM.
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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 165377-44-6 |
分子式 | C23H34Cl2N2O2 |
分子量 | 441.434 |
别名 | 库他美新二盐酸盐 ;SA4503 dihydrochloride;AGY94806 dihydrochloride;Cutamesine;AGY 94806;SA 4503;Cutamesine dihydrochloride |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -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 |
动物实验配方 |