LMPTP inhibitor 1

LMPTP inhibitor 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A. IC50 & Target: IC50: 0.8 μM (LMPTP-A)^[1] In Vitro: LMPTP inhibitor 1 (Compound 23) is a selective inhibitor of low molecular weight protein tyrosine phosphatase, with an IC₅₀ of 0.8 μM LMPTP-A and shows more potent effect on LMPTP-A versus LMPTP-B. LMPTP inhibitor 1 (10 μM) also enhances HepG2 IR phosphorylation after insulin stimulation in human HepG2 hepatocytes^[1]. In Vivo: LMPTP inhibitor 1 is orally bioavailable, and results in appr 680 nM mean serum concentration after treatment of 0.03% w/w, while treatment with 0.05% w/w results in >3 μM; also reverses diabetes in obese mice. LMPTP inhibitor 1 (0.05% w/w) inhibits LMPTP activity, significantly improves glucose tolerance and decreases fasting insulin levels of diabetic DIO mice, without affecting body weight^[1].