DPM-1001

目录号: PL09544
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。
CAS No. :1471172-27-6
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中文名称
DPM-1001
中文别名
化合物 T15166
英文名称
DPM-1001
英文别名
DPM-1001;CID 139291002;DPM-1001 (DPM1001);Cholan-24-oic acid, 7-hydroxy-3-[[4-[(2-pyridinylmethyl)amino]butyl]amino]-, methyl ester, (3α,5α,7α)-
Cas No.
1471172-27-6
分子式
C35H57N3O3
分子量
567.85
包装储存
Pure form -20°C 3 years;In solvent -80°C 6 months
详情描述
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。
产品详情
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 IC 50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property.
性状
Oil
IC50 & Target[1][2]
IC50: 100 nM (PTP1B)
体外研究(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). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Pure form -20°C 3 years;In solvent -80°C 6 months
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (176.10 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)
[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.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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