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。
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property[1].
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)[1].
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[1].
[1]. Krishnan N, et al. A potent, selective, and orally bioavailable inhibitor of the protein-tyrosine phosphatase PTP1B improves insulin and leptin signaling in animal models. J Biol Chem. 2018 Feb 2;293(5):1517-1525.
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