产品
编 号:F171065
分子式:C35H57N3O3
分子量:567.85
产品类型
结构图
CAS No: 1471172-27-6
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产品详情
生物活性:
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.
体内研究:
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.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.
体外研究:
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).