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DPM-1001 trihydrochloride

CAS No. :

MCE 站：DPM-1001 trihydrochloride

产品活性：DPM-1001 trihydrochloride 是一种有效的，特异性的，具有口服活性的，且非竞争性的蛋白酪氨酸磷酸酶 (PTP1B) 抑制剂，其 IC₅₀ 为 100 nM。DPM-1001 trihydrochloride 是特异性 PTP1B 抑制剂 MSI-1436 (IC₅₀=600 nM) 的类似物。DPM-1001 trihydrochloride 具有抗糖尿病特性。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphatase

In Vitro: DPM-1001 trihydrochloride inhibits the short form of PTP1B reversibly, whereas PTP1B(1–405) remained inactive over an extended period of time. DPM-1001 is against PTP1B(1–405) with no pre-incubation, the IC₅₀?value for PTP1B(1–405) is 600 nM. However, after a 30-min pre-incubation, the potency is improved to 100 nM. In contrast, there is no obvious time-dependent change in the IC₅₀?value for PTP1B(1–321).

In Vivo: DPM-1001 trihydrochloride (oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days) inhibits diet-induced obesity in mice by improving insulin and leptin signaling. DPM-1001 trihydrochloride-treated, high-fat diet-fed mice starts losing weight within 5 days of treatment. The weight loss continues for approximately 3 weeks, after which no further decrease in body weight is observed.

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