Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PTP1B-IN-3 diammonium is a highly effective and orally bioavailable inhibitor of the protein tyrosine phosphatase 1B (PTP1B) enzyme, with an IC50 value of 120 nM for both PTP1B and TCPTP. This compound exhibits potent antidiabetic and anticancer properties, as supported by extensive research [1] [2].
説明 | PTP1B-IN-3 diammonium is a highly effective and orally bioavailable inhibitor of the protein tyrosine phosphatase 1B (PTP1B) enzyme, with an IC50 value of 120 nM for both PTP1B and TCPTP. This compound exhibits potent antidiabetic and anticancer properties, as supported by extensive research [1] [2]. |
In vivo | In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) demonstrates a dose-dependent reduction of glucose levels, with 60%, 80%, and 100% inhibition observed at dosages of 1, 3, and 10 mg/kg, respectively, when administered orally 2 hours before a glucose challenge, showcasing an efficacious dose (ED 50) of 0.8 mg/kg. Furthermore, PTP1B-IN-3 effectively delays tumor onset in NDL2 Ptpn1 transgenic mice, extending the average period before tumor development from 28 to 75 days, when given orally at 30 mg/kg for 21 days. The compound also shows favorable pharmacokinetic properties in DIO mice, including good oral bioavailability (24%), slow clearance rate (0.71 mL/kg/min), and a substantial elimination half-life (6 hours). Although oral bioavailability decreases in higher species—rats (4%) and squirrel monkeys (2%)—remarkable exposure levels are still achieved with oral administration. |
分子量 | 396.12 |
分子式 | C12H13BrF2N3O3P |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
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PTP1B-IN-3 diammonium Others Inhibitor inhibitor inhibit