Description
Gemigliptin (LC15-0444 ) 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 exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.
Product information
CAS Number: 911637-19-9
Molecular Weight: 489.36
Formula: C18H19F8N5O2
Chemical Name: 1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-5H,6H,7H,8H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one
Smiles: N[C@@H](CC(=O)N1CC2=NC(=NC(=C2CC1)C(F)(F)F)C(F)(F)F)CN1CC(F)(F)CCC1=O
InChiKey: ZWPRRQZNBDYKLH-VIFPVBQESA-N
InChi: InChI=1S/C18H19F8N5O2/c19-16(20)3-1-12(32)31(8-16)6-9(27)5-13(33)30-4-2-10-11(7-30)28-15(18(24,25)26)29-14(10)17(21,22)23/h9H,1-8,27H2/t9-/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (102.17 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM. Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM. Gemigliptin is a competitive inhibitor with a Ki of 7.25 nM.
In Vivo:
Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo. Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.
Products are for research use only. Not for human use.
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