1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. 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.

Gemigliptin Chemical Structure

Gemigliptin Chemical Structure

CAS No. : 911637-19-9

Size Price Stock
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO USD 121 Ask For Quote & Lead Time
Solid
5 mg USD 70 Ask For Quote & Lead Time
10 mg USD 110 Ask For Quote & Lead Time
50 mg USD 330 Ask For Quote & Lead Time
100 mg USD 520 Ask For Quote & Lead Time

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Description

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[1][2].

IC50 & Target

IC50: 10.3 nM (human recombinant DPP-4)[2]

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 (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo[1].
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.

Animal Model: Male C57BL/KsJ-db/db mice (7 weeks old)[1]
Dosage: 100 mg/kg
Administration: Oral gavage, daily, for 12 weeks
Result: Significantly reduced circulating AGE levels by 44.5% in serum.
Clinical Trial
Molecular Weight

489.36

Formula

C18H19F8N5O2

CAS No.
Appearance

Solid

Color

White to orange

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

Shipping

Room temperature in continental US; may vary elsewhere.

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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 4.0870 mL
View the Complete Stock Solution Preparation Table
  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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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Gemigliptin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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