PTP1B/AKR1B1-IN-1

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PTP1B/AKR1B1-IN-1

CAS No. :

MCE 国际站：PTP1B/AKR1B1-IN-1

产品活性：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-PTP，IC₅₀ 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。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphatase  |  Aldose Reductase

In Vitro: PTP1B/AKR1B1-IN-1 (compound 6f) tightly binds to PTP1B and AKR1B1 with K_i values of 4.6 μM, and 0.08 μM, respectively.
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) shows insignificant cytotoxicity in differentiated murine C2C12 cells.
PTP1B/AKR1B1-IN-1 (20 μM; 24 h) enhances the increases of Akt phosphorylation in murine C2C12 cell line with insulin (10 μM; 15 min).
PTP1B/AKR1B1-IN-1 (2 μM; 24 h) results significant impairment of sorbitol accumulation in human lens epithelial line B3 (HLE) cells, induced with 75 mM d-glucose for 24 h.

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