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.

Product information

CAS Number: 1374639-74-3

Molecular Weight: 639.45

Formula: C22H25F8N5O8

Chemical Name: (2R,3R)-2,3-dihydroxybutanedioic acid; 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.OC(=O)[C@H](O)[C@@H](O)C(O)=O

InChiKey: DPEZWSNXONTJHT-NDAAPVSOSA-N

InChi: InChI=1S/C18H19F8N5O2.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h9H,1-8,27H2;1-2,5-6H,(H,7,8)(H,9,10)/t9-;1-,2-/m01/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (156.38 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 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.

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.

Products are for research use only. Not for human use.