Gemigliptin

SKU: orb1299878

Description

Gemigliptin (LC15-0444) is a highly potent and selective DPP-4 inhibitor with a KD of 7.25 nM. It is a valuable research tool for studying type 2 diabetes, utilized in both in vitro enzymatic assays and in vivo models of hyperglycemia.

Research Area

Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 911637-19-9
• MW: 489.36
• Purity: 99.33% (May vary between batches)
• Formula: C₁₈H₁₉F₈N₅O₂
• SMILES: N[C@H](CN1CC(F)(F)CCC1=O)CC(=O)N1CCc2c(C1)nc(nc2C(F)(F)F)C(F)(F)F
• Target: DPP-4,Proteasome
• Solubility: DMSO:122.5 mg/mL (250.33 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.17 mM)

Bioactivity

• Target IC50:
  DPP4:7.25 nM(KD)
• In Vitro:
  Gemigliptin attenuated vascular calcification and osteogenic trans-differentiation in vascular smooth muscle cells via multiple steps including downregulation of PiT-1 expression and suppression of reactive oxygen species generation, phospho-PI3K/AKT, and the Wnt signaling pathway.Gemigliptin treatment attenuated phosphorylated nuclear factor-κB levels, which had been increased in the UUO kidney as well as in TGF-β-treated cultured renal cells.
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• Cell Research:
  Using immunohistochemical and Western blot analysis, Quantitated components of the NLRP3 inflammasome in kidneys with and without gemigliptin treatment, and in vitro in human kidney tubular epithelial human renal proximal tubule cells (HK-2) cells, further analyzed the effect of gemigliptin on transforming growth factor-β (TGF-β)-stimulated production of profibrotic proteins.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dipeptidyl Peptidase, DPP-4, DPP4, DPP, Inhibitor, inhibit, Gemigliptin, LC15-0444

Compound Identifiers

PubChem CID

11953153