PTP1B-IN-3 diammonium |
Catalog No.GC63705 |
PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s 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 ED50 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 (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[1].
[1]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.
[2]. Price N, et al. Safety and Efficacy of a Topical Sodium Channel Inhibitor (TV-45070) in Patients With Postherpetic Neuralgia (PHN): A Randomized, Controlled, Proof-of-Concept, Crossover Study, With a Subgroup Analysis of the Nav1.7 R1150W Genotype. Clin J Pain. 2017 Apr;33(4):310-318.
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(Based on Reviews and 33 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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