Trodusquemine
中文名称 | Trodusquemine |
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中文同义词 | 化合物 T12116 |
英文名称 | MSI-1436 |
英文同义词 | MSI-1436;Trodusquemine;TRODUSQUEMINE;AMINOSTEROL-1436;MSI1436;Cholestane-7,24-diol, 3-[[3-[[4-[(3-aminopropyl)amino]butyl]amino]propyl]amino]-, 24-(hydrogen sulfate), (3β,5α,7α,24R)-;Trodusquemine (MSI-1436);MSI-1436 USP/EP/BP;MSI-1436(Trodusquemine;MSI 1436,MSI1436 |
CAS号 | 186139-09-3 |
分子式 | C37H72N4O5S |
分子量 | 685.07 |
EINECS号 | |
相关类别 | |
Mol文件 | 186139-09-3.mol |
结构式 |
Trodusquemine 性质
密度 | 1.12±0.1 g/cm3(Predicted) |
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储存条件 | 2-8°C(protect from light) |
溶解度 | 溶于二甲基亚砜 |
酸度系数(pKa) | -3.49±0.18(Predicted) |
形态 | 固体 |
颜色 | 白色至黄色 |
IC50: 1 μM (PTB1B), 224 μM (TCPTP)
In HepG2, MSI-1436 (10 µM, 30 min) alone has no effect on phosphorylation of IRβ, but in conjunction with 100 nM insulin, MSI-1436 increases p-IRβ 18-fold over untreated cells and by approximately threefold over cells treated with insulin alone. MSI-1436's inhibition of TCPTP is approximately two logs less than the effect on PTP1B activity, with a resulting IC 50 value of 224 µM. MSI-1436 (Trodusquemine, 10 μM) restores ERK phosphorylation in response to mGluR1/5 agonist DHPG in F11 neuronal cells. MSI-1436 (10 uM) rescues DHPG-induced holding currents and restores DSI in LMO4KO BLA neurons. MSI-1436 (0.1-100 µM) blocks PTP1B activity, has insulin-mimetic effects in cultured neuronal cells.
MSI-1436 (10 mg/kg, i.p.) causes obesity-dependent body weight, reduces total body fat content and adipocyte size and lipid content of white adipose tissue of mice. MSI-1436 treatment significantly reduces plasma insulin levels. MSI-1436 (10 mg/kg, i.p.) increases phosphorylation of STAT-3 2.7-fold and, in conjunction with 100 U/kg insulin, p-IRβ increases threefold over insulin alone-treated rats. MSI-1436 (Trodusquemine) exhibits anxiolytic effect through a restoration of endocannabinoid (eCB) signaling within the amygdala. MSI-1436 (5 mg/kg, i.p.) has an anti-diabetic effect on diabetic mice, and is sufficient to suppress food intake and cause weight loss in CD1 mice.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-12219 | MSI-1436 | 500 μg | 3000元 | |
2022/09/18 | HY-12219 | Trodusquemine MSI-1436 | 186139-09-3 | 1mg | 5000元 |