DPM-1001 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 是特异性 PTP1B 抑制剂 MSI-1436 (IC50=600 nM) 的类似物。DPM-1001 具有抗糖尿病特性。
| 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). |
|||||||||
| 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.
|
|||||||||
| 分子量 |
567.85
|
|||||||||
| CAS号 |
1471172-27-6
|
|||||||||
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
|||||||||
| 储存方式 |
|
关注我们
获得KKL MED 最新资讯
客服小K 
客服小K
Data Sheet