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

Gemigliptin (Synonyms: LC15-0444)

Cat. No.: HY-14892 Purity: 98.31%
Handling Instructions

Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.

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

Gemigliptin Chemical Structure

Gemigliptin Chemical Structure

CAS No. : 911637-19-9

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Description

Gemigliptin is a highly selective dipeptidyl peptidase 4 (DPP4) inhibitor with a KD of 7.25 nM.

IC50 & Target

Ki: 7.25 nM (DPP4)[1]

In Vitro

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].

In Vivo

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].

Clinical Trial
Molecular Weight

489.36

Formula

C₁₈H₁₉F₈N₅O₂

CAS No.

911637-19-9

SMILES

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 : ≥ 122.5 mg/mL (250.33 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2043 mL 1.0217 mL 2.0435 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

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].

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

Animal Administration

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].

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

References
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Gemigliptin
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HY-14892
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