| Description | Gemigliptin Tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). It has an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. |
| In vitro | Gemigliptin tartrate通过抑制AGE-BSA的形成,其IC50为11.69 mM[1]。此外,Gemigliptin tartrate还能抑制预形成的AGE-BSA与大鼠尾腱胶原的交联,IC50为1.39 mM[1]。Gemigliptin tartrate是一种具有7.25 nM Ki值的竞争性DPP-4抑制剂[2]。 |
| In vivo | Gemigliptin tartrate 在体内抑制了AGEs的形成以及AGE交联[1]。Gemigliptin tartrate 以剂量依赖的方式抑制了大鼠、狗和猴子的血浆DPP-4活性[2]。 |
| Target activity | DPP4 (human recombinant):10.3 nM |
| Synonyms | 吉格列汀酒石酸盐, LC15-0444 tartrate |
| molecular weight | 639.45 |
| Molecular formula | C22H25F8N5O8 |
| CAS | 1374639-74-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 90 mg/mL (140.75 mM), Sonication is recommended. |
| References | 1. Jung E , Kim J , Kim S H , et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo.[J]. European Journal of Pharmacology, 2014, 744:98-102. 2. Kim S H , Jung E , Yoon M K , et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo[J]. European Journal of Pharmacology, 2016, 788:54-64. |