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

Gemigliptin tartrate (Synonyms: LC15-0444 tartrate)

Cat. No.: HY-14892A Purity: 98.28%
Handling Instructions

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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10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 110 In-stock
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50 mg USD 330 In-stock
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100 mg USD 520 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

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.

1374639-74-3

SMILES

O=C(O)[[email protected]](O)[[email protected]@H](O)C(O)=O.O=C1N(C[[email protected]@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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (156.38 mM; Need ultrasonic)

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
10 mM 0.1564 mL 0.7819 mL 1.5638 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are provided by MCE.
References
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Keywords:

GemigliptinLC15-0444Dipeptidyl PeptidaseDPPdipeptidylpeptidase-4glycationadvancedendproductsAGEtype2diabetesmellitusInhibitorinhibitorinhibit

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Product Name:
Gemigliptin tartrate
Cat. No.:
HY-14892A
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