Gemigliptin
Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Gemigliptin tartrate) that retains the same biological activity.
For research use only. We do not sell to patients.
- CAS No.: 911637-19-9
- Formula: C18H19F8N5O2
- Molecular Weight:489.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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HY-13233A
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SaxagliptinDPP-4 Inhibitor -
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TrelagliptinDPP-4 Inhibitor -
HY-15408A
Trelagliptin succinateDPP-4 Inhibitor -
HY-A0023A
AlogliptinDPP-4 Inhibitor -
HY-14806
TeneligliptinDPP-4 Inhibitor -
HY-14877
AnagliptinDPP-4 Inhibitor -
HY-10284
LinagliptinDPP-4 Inhibitor -
HY-10285A
Saxagliptin hydrateDPP-4 Inhibitor -
HY-14291
VildagliptinDPP-IV Inhibitor -
HY-A0023
Alogliptin BenzoateDPP-4 Inhibitor -
HY-15981
OmarigliptinDPP-4 Inhibitor
Biological Activity
Description
IC50 & Target
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DPP-4 |
In Vitro
Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1].
Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM[1].
Gemigliptin is a competitive inhibitor with a Ki of 7.25 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/KsJ-db/db mice (7 weeks old)[1]
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Dosage:100 mg/kg
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Administration:Oral gavage, daily, for 12 weeks
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Result:Significantly reduced circulating AGE levels by 44.5% in serum.
Chemical Information
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CAS No. 911637-19-9
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Appearance Solid
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Molecular Weight 489.36
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Formula C18H19F8N5O2
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Color White to orange
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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
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Synonyms
LC15-0444
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (102.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
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Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0435 mL | 10.2174 mL | 20.4349 mL | 51.0871 mL |
| 5 mM | 0.4087 mL | 2.0435 mL | 4.0870 mL | 10.2174 mL | |
| 10 mM | 0.2043 mL | 1.0217 mL | 2.0435 mL | 5.1087 mL | |
| 15 mM | 0.1362 mL | 0.6812 mL | 1.3623 mL | 3.4058 mL | |
| 20 mM | 0.1022 mL | 0.5109 mL | 1.0217 mL | 2.5544 mL | |
| 25 mM | 0.0817 mL | 0.4087 mL | 0.8174 mL | 2.0435 mL | |
| 30 mM | 0.0681 mL | 0.3406 mL | 0.6812 mL | 1.7029 mL | |
| 40 mM | 0.0511 mL | 0.2554 mL | 0.5109 mL | 1.2772 mL | |
| 50 mM | 0.0409 mL | 0.2043 mL | 0.4087 mL | 1.0217 mL | |
| 60 mM | 0.0341 mL | 0.1703 mL | 0.3406 mL | 0.8515 mL | |
| 80 mM | 0.0255 mL | 0.1277 mL | 0.2554 mL | 0.6386 mL | |
| 100 mM | 0.0204 mL | 0.1022 mL | 0.2043 mL | 0.5109 mL |
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