General description

Claramine is an easy and quick to synthesize polyaminosteroid derivative. It is a trodusquemine-related compound and shares with it a spermino group, which is responsible for its inhibitory action towards protein tyrosine phosphatase 1B (PTP1B).

Biochem/physiol Actions

Claramine is a more conveniently-manufactured lead compound for the derivation of therapeutic agents. It is believed to be useful for the treatment of type II diabetes. Claramine is capable of crossing blood brain barrier (BBB) and is thought to mediate its action through hypothalamus, which is responsible for maintaining metabolic homeostasis. Claramine A1 is found effective against multidrug resistant bacteria and nosocomial diseases.

Claramine is a protein tyrosine phosphatase 1B (PTP1B) inhibitor, an analog of Trodusquemine. Like Trodusquemine, Claramine is a selective inhibitor of protein tyrosine phosphatase 1B (PTB1B), and not its closest related phosphatase TC-PTP. Claramine activated insulin signaling, increasing phosphorylation of insulin receptor-β (IRβ), Akt and GSK3β. It improved insulin sensitivity, restoring glycemic control in diabetic mice, and caused weight loss by suppressing food intake.