2. Metabolic Enzyme/Protease
  3. Phosphatase
  4. MSI-1436

MSI-1436  (Synonyms: Trodusquemine; Aminosterol-1436)

目录号: HY-12219
COA 产品使用指南 技术支持

MSI-1436 是具有选择性的 PTP1B 的非竞争性抑制剂，其 IC50 为 1 μM，而对 TCPTP 的 IC50 值为 224 μM。

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MSI-1436 Chemical Structure

MSI-1436 Chemical Structure

CAS No. : 186139-09-3

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规格 价格 是否有货
500 μg ￥3000
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MSI-1436 的其他形式现货产品:

Customer Review

Other Forms of MSI-1436:

MSI-1436 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).

IC50 & Target

IC50: 1 μM (PTB1B), 224 μM (TCPTP)[1]
体外研究
(In Vitro)

在 HepG2 中，单独的 MSI-1436 (10 μM，30 分钟) 对 IRβ 的磷酸化没有影响，但与 100 nM 胰岛素联合使用时，MSI-1436 使 p-IRβ 比未处理的细胞高 18 倍，比处理过的细胞高约三倍单独使用胰岛素。MSI-1436 对 TCPTP 的抑制比对 PTP1B 活性的影响低约两个对数，由此产生的 IC50 值为 224 μM[1]。MSI-1436 (Trodusquemine，10 μM) 在 F11 神经元细胞中恢复 ERK 磷酸化以响应 mGluR1/5 激动剂 DHPG。MSI-1436 (10 uM) 挽救 DHPG 诱导的保持电流并恢复 LMO4KO BLA 神经元中的 DSI[2]。MSI-1436 (0.1-100 μM) 阻断 PTP1B 活性，在培养的神经元细胞中具有胰岛素样作用[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MSI-1436 相关抗体:
体内研究
(In Vivo)

MSI-1436 (10 mg/kg，ip) 导致肥胖依赖性体重，降低小鼠的全身脂肪含量和脂肪细胞大小以及白色脂肪组织的脂质含量。MSI-1436 处理可显著降低血浆胰岛素水平。MSI-1436 (10 mg/kg，腹腔注射) 使 STAT-3 的磷酸化增加 2.7 倍，与 100 U/kg 胰岛素联合使用时，p-IRβ 比单独使用胰岛素处理的大鼠增加三倍[1]。MSI-1436 (Trodusquemine) 通过恢复杏仁核内的内源性大麻素 (eCB) 信号而表现出抗焦虑作用[2]。MSI-1436 (5 mg/kg，ip) 对糖尿病小鼠具有抗糖尿病作用，足以抑制 CD1 小鼠的食物摄入并导致体重减轻[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

685.06

Formula

C37H72N4O5S
CAS 号
性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: ≥95.0%

COA (263 KB) HNMR (205 KB)

产品使用指南 (1538 KB)
参考文献
Animal Administration
[1]

Mice
Male AKR/J mice are randomLy placed on ad libitum 10, 45, or 60% fat kcal diets. After -14 weeks, mice are randomly assigned to three treatment groups (n=5-8 mice/group); MSI-1436 (initial dose of 10 mg/kg with three subsequent weekly doses of 5 mg/kg, intraperitoneally), vehicle (saline, 10 mL/kg, weekly 4×), or pair-fed (PF). PF animals are injected with saline (weekly 4×) and allotted the amount of food consumed daily by MSI-1436-treated animals. On day 23, mice are anesthetized and euthanized for blood and tissue collection, respectively. Plasma is obtained following centrifugation of blood 14,000 rpm for 10 min at 4°C.
Rats
Nine-week-old male Sprague-Dawley rats (225-260 g) with ad libitum access to normal rodent chow are dosed intraperitoneally with MSI-1436 (10 mg/kg, IP) or saline. After an overnight fast, the rats are dosed intraperitoneally with saline or 100 U/kg of insulin. At 30 min after dose, animals are killed, and hypothalami are harvested and homogenized in 1 mL of tissue extraction reagent plus phosphatase and protease inhibitors. Samples are centrifuged (14,000 rpm for 10 min at 4°C), and the protein content of the supernatants are quantitated via BCA kit.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

MSI-1436 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MSI-1436186139-09-3Trodusquemine Aminosterol-1436MSI1436MSI 1436Aminosterol1436Aminosterol 1436Aminosterol-1436PhosphataseInhibitorinhibitorinhibit

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