Bis(maltolato)oxovanadium(IV)

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer[1][2].

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

Research Areas >> Metabolic Disease

IC50: 126 nM (HCPTPA), 109 nM (PTP1B), 26 nM (HPTPβ) and 201 nM (SHP2)[2]

Bis(maltolato)oxovanadium(IV) treatment enhances the phosphorylation of the insulin receptor and of the insulin signalling key intermediate Akt. Bis(maltolato)oxovanadium(IV) (BMOV; 50 μM) treatment also resultes in an increased glucose uptake in C2C12 cells[1].

Bis(maltolato)oxovanadium(IV) (BMOV; 0.75-3.0 mmol; intraperitoneal injection; twice weekly; for 6 weeks; C57BL/6J mice) treatment ameliorates the metabolic phenotype. Liver, skeletal muscle, and adipose tissue revealed a significantly reduced PTP activity in all analysed tissues compared to HFD mice[1]. Animal Model: C57BL/6J mice (4-6 weeks) fed with high-fat diet (HFD)[1] Dosage: 0.75-3.0 mmol Administration: Intraperitoneal injection; twice weekly; for 6 weeks Result: Ameliorated the metabolic phenotype, as evidenced by reduced body weight, improved insulin sensitivity and glucose tolerance.

[1]. Janine Krüger, et al. Inhibition of Src homology 2 domain-containing phosphatase 1 increases insulin sensitivity in high-fat diet-induced insulin-resistant mice. FEBS Open Bio. 2016 Jan 4;6(3):179-89.

[2]. Kevin G Peters, et al. Mechanism of insulin sensitization by BMOV (bis maltolato oxo vanadium); unliganded vanadium (VO4) as the active component. J Inorg Biochem. 2003 Aug 1;96(2-3):321-30.