| Description | MSI-1436 is a selective, non-competitive the enzyme protein-tyrosine phosphatase 1B (PTB1B)inhibitor(IC50 of appr 1 μM) |
| In vitro | Trodusquemine significantly enhanced insulin-stimulated tyrosine phosphorylation of insulin receptor (IR) beta and STAT3, direct targets of PTP1B, in HepG2 cells in vitro and/or hypothalamic tissue[1]. |
| In vivo | Trodusquemine (MSI-1436) causes rapid and reversible weight loss in genetic models of obesity.?Trodusquemine suppressed appetite, reduced body weight (BW) in a fat-specific manner, and improved plasma insulin and leptin levels in mice[1]. |
| Target activity | PTB1B:1 μM , TCPTP:224 μM |
| Synonyms | Aminosterol-1436, Trodusquemine |
| molecular weight | 685.06 |
| Molecular formula | C37H72N4O5S |
| CAS | 186139-09-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Lantz KA, et al. Inhibition of PTP1B by trodusquemine (MSI-1436) causes fat-specific weight loss in diet-induced obese mice. Obesity (Silver Spring). 2010 Aug;18(8):1516-1523. 2. Qin Z, et al. Chronic stress induces anxiety via an amygdalar intracellular cascade that impairs endocannabinoid signaling. Neuron. 2015 Mar 18;85(6):1319-31. 3. Qin Z, et al. Functional properties of Claramine: a novel PTP1B inhibitor and insulin-mimetic compound. Biochem Biophys Res Commun. 2015 Feb 27;458(1):21-7. |