购物车
- 全部删除
- 您的购物车当前为空
Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂,IC50值为 17.4 nM。
为众多的药物研发团队赋能,
让新药发现更简单!
Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂,IC50值为 17.4 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 268 | 现货 | |
2 mg | ¥ 378 | 现货 | |
5 mg | ¥ 613 | 现货 | |
10 mg | ¥ 988 | 现货 | |
25 mg | ¥ 1,670 | 现货 | |
50 mg | ¥ 2,480 | 现货 | |
100 mg | ¥ 3,690 | 现货 | |
500 mg | ¥ 8,250 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 712 | 现货 |
产品描述 | Cutamesine dihydrochloride (SA4503 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. |
靶点活性 | σ1:17.4 nM |
体外活性 | Sigma受体可能涉及中枢神经系统的多种疾病。Cutamesine,一种强效的σ1受体激动剂,在豚鼠脑膜中对σ1的亲和力(IC50=17.4 nM)高出σ2(IC50=1,784 nM)103倍。在豚鼠脑匀浆中,Cutamesine对σ1(Ki=4.6 nM)的选择性比对σ2(Ki=63.1 nM)高14倍[1]。Cutamesine能保护运动神经元NSC34细胞免受超氧化物歧化酶1和无血清的神经毒性损害。它提高Akt和细胞外信号调节激酶(ERK)1/2的磷酸化水平[2]。Cutamesine降低MAPK/ERK途径的激活,并下调离子型谷氨酸受体,GluR1的表达[3]。 |
体内活性 | SA4503延长了SOD1 g93A小鼠[2]的存活时间。 |
细胞实验 | 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 SA4503 at a final concentration of 1, 3, or 10 nM[2]. |
别名 | 库他美新二盐酸盐, SA4503 dihydrochloride, SA4503 (dihydrochloride), AGY94806 dihydrochloride |
分子量 | 441.43 |
分子式 | C23H32N2O2·2HCl |
CAS No. | 165377-44-6 |
Smiles | Cl.Cl.COc1ccc(CCN2CCN(CCCc3ccccc3)CC2)cc1OC |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | DMSO: 10 mg/mL (22.65 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
|
版权所有©2015-2024 TargetMol Chemicals Inc.保留所有权利.
评论内容