| 规格 | 价格 | 库存 | 数量 | 操作 |
|---|---|---|---|---|
| 10mg | ¥982.00 | 现货 | 1 | |
| 50mg | ¥2,945.00 | 现货 | 1 | |
| 100mg | ¥4,641.00 | 现货 | 1 | |
| 10mM (in 1mL DMSO) | ¥1,079.00 | 现货 | 1 |
Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.
[1] Sung-Ho Kim, et al. Eur J Pharmacol. 2016 Oct 5;788:54-64. [2] Sung-Ho Kim, et al. Arch Pharm Res. 2013 Oct;36(10):1185-8.
Kinase experiment: | The enzyme kinetic analysis of gemigliptin on DPP-4 is performed using a continuous spectrophotometric assay with the substrate Gly-Pro-pNA. Briefly, inhibition of DPP-4 activity is determined by measuring the absorbance (at 390 nm) resulting from the cleavage of the substrate Gly-Pro-pNA by the DPP-4 enzyme under steady-state conditions. Enzyme activity is defined as the slope (in mOD/ min) from 5 to 15 min. The inhibition pattern is evaluated using a Lineweaver-Burk plot, and the Ki is determined using a curve- fitting program[2]. |
Animal experiment: | Mice[1]Seven week-old male C57BL/KsJ-db/db mice and their lean littermates (db/þ, normal) are randomly assigned to three (n=10) groups. One group of db/db mice is orally administered gemigliptin (100 mg/kg body weight) and another group is administered the same amount of vehicle via oral gavage for 12 weeks. Non-diabetic littermates receive the same vehicle treatment. Blood glucose level and body weight are measured weekly[1]. |
References: [1]. Jung E, et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102. |
