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。

PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC 50 s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 diammonium has antidiabetic and anticancer effects [1] [2].

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].

C12H13BrF2N3O3P

396.12

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years