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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].
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].
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
25 mg | ¥ 29,700 | 5日内发货 |
产品描述 | 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]. |
体内活性 | 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 ED 50 of 0.8 mg/kg [1]. 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 [1]. 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 [1]. |
分子量 | 396.12 |
分子式 | C12H13BrF2N3O3P |
存储 | Shipping with blue ice. |
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