PTP1B-IN-3

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PTP1B-IN-3 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 具有抗糖尿病和抗癌作用。

PTP1B-IN-3 is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 has antidiabetic and anticancer effects.

——

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 (t1/2 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.

——

Metabolic Enzyme/Protease

Phosphatase

Phosphatase

——

——

809272-64-8

362.06

C12H7BrF2NO3P

>98% (HPLC)

——

N#CC=1C=CC2=CC(Br)=C(C=C2C1)C(F)(F)P(=O)(O)O

——

(-20℃)

With Ice Pack

≥ 2 years