CAS 945667-22-1 Purity >99.0% (HPLC) API

API (CAS: 945667-22-1) is a selective and reversible dipeptidyl peptidase-4 (DPP4) inhibitor that may be used to develop treatment for type 2 diabetes. It is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM. Target: DPP4 in vitro: It has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than Sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, It demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of it is two-fold less potent than the parent. Both (CAS: 945667-22-1) and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases. (CAS: 945667-22-1) reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: It is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls.