PTP1B-IN-3 diammonium,2702673-

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PTP1B-IN-3 diammonium

CAS No. : 2702673-78-5

MCE 国际站：PTP1B-IN-3 diammonium

产品活性：PTP1B-IN-3 diammonium 是有效的，有选择性的 PTP1B 抑制剂，对 PTP1B 和 TCPTP 的 IC₅₀ 值均为 120 nM。PTP1B-IN-3 diammonium 具有抗糖尿病和抗癌作用。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphatase

In Vivo: In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED₅₀ of 0.8 mg/kg.
In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1^+/+ mice, extending the median tumor free days (T50) from 28 days to 75 days.
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t_1/2 of 6 h). The oral bioavailability in higher species such as rats (F of 4%) and squirrel monkeys (F of 2%) are substantially lower but excellent exposures are achieved with oral dosing.

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