186139-09-3
基本信息
Trodusquemine
MSI-1436 USP/EP/BP
Trodusquemine (MSI-1436)
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)-
物理化学性质
| 密度 | 1.12±0.1 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Sealed in dry,2-8°C |
| 溶解度 | Soluble in DMSO |
| 酸度系数(pKa) | -3.49±0.18(Predicted) |
| 形态 | Solid |
| 颜色 | White to yellow |
常见问题列表
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.