Gemigliptin (LC15-0444) |
| Catalog No.GC33769 |
La gemigliptine (LC15-0444) (LC15-0444) est un inhibiteur hautement sélectif, réversible et compétitif de la dipeptidyl peptidase-4 (DPP-4), avec une IC50 de 10,3 nM pour la DPP-4 recombinante humaine.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 911637-19-9
Sample solution is provided at 25 µL, 10mM.
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Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.
In in vitro assay, gemigliptin dose-dependently inhibits methylglyoxal-modified AGE-bovine serum albumin (BSA) formation (IC50=11.69 mM). AGE-collagen cross-linking assays shows that gemigliptin has a potent inhibitory effect (IC50=1.39 mM) on AGE-BSA cross-links to rat tail tendon collagen. In addition, gemigliptin directly traps methylglyoxal in a concentration-dependent manner[1]. Gemigliptin is a reversible and competitive inhibitor with a Ki value of 7.25±0.67 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[2].
Administration of gemigliptin supressed elevated serum levels of advanced glycation end products (AGE) in type 2 diabetic db/db mice. In mice and dogs, gemigliptin prevents the degradation of active glucagon-like peptide-1 by DPP-4 inhibition, which improves glucose tolerance by increasing insulin secretion and reducing glucagon secretion during an oral glucose tolerance test[2].
[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. [2]. Kim SH, et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur J Pharmacol. 2016 Oct 5;788:54-64.
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. | |
| Cas No. | 911637-19-9 | SDF | |
| Canonical SMILES | O=C1N(C[C@@H](N)CC(N2CCC3=C(C(F)(F)F)N=C(C(F)(F)F)N=C3C2)=O)CC(F)(F)CC1 | ||
| Formula | C18H19F8N5O2 | M.Wt | 489.36 |
| Solubility | DMSO : ≥ 122.5 mg/mL (250.33 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0435 mL | 10.2174 mL | 20.4349 mL |
| 5 mM | 0.4087 mL | 2.0435 mL | 4.087 mL |
| 10 mM | 0.2043 mL | 1.0217 mL | 2.0435 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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