DPM-1001

DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC₅₀ of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property^[1]. IC50 & Target: IC50: 100 nM (PTP1B)^[1] In Vitro: DPM-1001 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]. In Vivo: DPM-1001 (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-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].