1. Metabolic Enzyme/Protease
  2. Phosphatase Aldose Reductase
  3. PTP1B/AKR1B1-IN-1

PTP1B/AKR1B1-IN-1 是蛋白酪氨酸磷酸酶 1B (PTP1B) 和醛糖还原酶 (AKR1B1) 的双重抑制剂,IC50 分别为 0.06 μM 和 4.3 μM。PTP1B/AKR1B1-IN-1 还抑制 TC-PTPIC50 为 9 μM。PTP1B/AKR1B1-IN-1 在小鼠成肌细胞中用作胰岛素模拟剂,并减少 AKR1B1 依赖性山梨糖醇的积累。PTP1B/AKR1B1-IN-1 可抑制 2 型糖尿病 (T2DM) 的发展以控制血糖水平。

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PTP1B/AKR1B1-IN-1 Chemical Structure

PTP1B/AKR1B1-IN-1 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PTP1B/AKR1B1-IN-1 is a dual inhibitor of protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM and 4.3 μM, respectively. PTP1B/AKR1B1-IN-1 also inhibits TC-PTP with an IC50 value of 9 μM. PTP1B/AKR1B1-IN-1 serves as an insulin-mimetic agent in murine myoblasts, and reduces AKR1B1-dependent sorbitol accumulation. PTP1B/AKR1B1-IN-1 inhibits development of type 2 diabetes mellitus (T2DM) to control blood glucose levels[1].

IC50 & Target

IC50: 0.06 μM (Protein tyrosine phosphatase 1B, PTP1B); 4.3 μM (Aldose reductase, AKR1B1); 9 μM (TC-PTP)[1]

体外研究
(In Vitro)

PTP1B/AKR1B1-IN-1 (化合物 6f) 与 PTP1B 和 AKR1B1 紧密结合,Ki 值分别为 4.6 μM 和 0.08 μM。 PTP1B/AKR1B1-IN-1 (20 μM;24 小时) 在分化的小鼠 C2C12 细胞中表现出微不足道的细胞毒性[1]
PTP1B/AKR1B1-IN-1 (20 μM;24 小时) 用胰岛素(10 μM;15 分钟)增强鼠类 C2C12 细胞系中 Akt 磷酸化的增加[1]
PTP1B/AKR1B1-IN-1 (2 μM;24 小时) 导致山梨糖醇在人晶状体上皮细胞系 B3 (HLE) 细胞中的积累显着受损。实验中,可同时用 75 mM D-葡萄糖诱导 24 小时[1]

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

Western Blot Analysis[1]

Cell Line: Murine C2C12 cell
Concentration: 20 μM; with or without 10 μM insulin for 15 min
Incubation Time: 24 h
Result: Increased Akt phosphorylation, and was enhanced by insulin.
分子量

427.54

Formula

C22H21NO4S2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

PTP1B/AKR1B1-IN-1 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.

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产品名称:
PTP1B/AKR1B1-IN-1
目录号:
HY-149254
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