Gemigliptin Tartrate(911637-19-9 free base)

SKU: orb1218881

Description

Gemigliptin tartrate is a highly selective, reversible and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). It has an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties.

Key Properties

• CAS Number: 1374639-74-3
• MW: 639.45
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₅F₈N₅O₈
• SMILES: O=C([C@@H]([C@H](C(O)=O)O)O)O.O=C1N(CC(F)(CC1)F)C[C@H](CC(N2CCC3=C(N=C(N=C3C2)C(F)(F)F)C(F)(F)F)=O)N
• Target: DPP
• Solubility: DMSO:90mg/ml(140.75mM; need ultrasonic)

Bioactivity

• In Vivo:
  Gemigliptin tartrate (100 mg/kg; i. g. ; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links In vivo. Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys. Animal model: Male C57BL/KsJ-db/db mice (7 weeks old). Dosage: 100 mg/kg. Administration: Oral gavage, daily, for 12 weeks. Result: Significantly reduced circulating AGE levels by 44.5% in serum.
• In Vitro:
  Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM. Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM. Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Ki of 7.25 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LC15-0444 tartrate

Quick Database Links

Gene Symbol

DPP