2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Gemigliptin tartrate

Gemigliptin tartrate  (Synonyms: LC15-0444 tartrate)

Cat. No.: HY-14892A Purity: 98.17%
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Gemigliptin tartrate (LC15-0444 tartrate) 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 tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

For research use only. We do not sell to patients.

Gemigliptin tartrate Chemical Structure

Gemigliptin tartrate Chemical Structure

CAS No. : 1374639-74-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 110 In-stock
50 mg USD 330 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Gemigliptin tartrate:

Gemigliptin tartrate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Gemigliptin tartrate (LC15-0444 tartrate) 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 tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate 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 tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1].
Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM[1].
Gemigliptin tartrate is a competitive DPP-4 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.

Gemigliptin tartrate Related Antibodies
In Vivo

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

639.45

Formula

C22H25F8N5O8
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

O=C(O)[C@H](O)[C@@H](O)C(O)=O.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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (156.38 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 1.5638 mL 7.8192 mL 15.6384 mL
5 mM 0.3128 mL 1.5638 mL 3.1277 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (3.91 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 (3.91 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5638 mL 7.8192 mL 15.6384 mL 39.0961 mL
5 mM 0.3128 mL 1.5638 mL 3.1277 mL 7.8192 mL
10 mM 0.1564 mL 0.7819 mL 1.5638 mL 3.9096 mL
15 mM 0.1043 mL 0.5213 mL 1.0426 mL 2.6064 mL
20 mM 0.0782 mL 0.3910 mL 0.7819 mL 1.9548 mL
25 mM 0.0626 mL 0.3128 mL 0.6255 mL 1.5638 mL
30 mM 0.0521 mL 0.2606 mL 0.5213 mL 1.3032 mL
40 mM 0.0391 mL 0.1955 mL 0.3910 mL 0.9774 mL
50 mM 0.0313 mL 0.1564 mL 0.3128 mL 0.7819 mL
60 mM 0.0261 mL 0.1303 mL 0.2606 mL 0.6516 mL
80 mM 0.0195 mL 0.0977 mL 0.1955 mL 0.4887 mL
100 mM 0.0156 mL 0.0782 mL 0.1564 mL 0.3910 mL
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Gemigliptin tartrate 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.

Keywords:

Gemigliptin1374639-74-3LC15-0444Dipeptidyl PeptidaseDPPdipeptidylpeptidase-4glycationadvancedendproductsAGEtype2diabetesmellitusInhibitorinhibitorinhibit

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