DPM-1001

DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC 50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property 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 IC 50 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 IC 50 value for PTP1B(1–321). MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J) Dosage: 5 mg/kg Administration: Oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days Result: Led to an 5% decrease in body weight. Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo . Form:Solid IC50& Target:IC50: 100 nM (PTP1B)

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