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Gemigliptin tartrate

Names

[ CAS No. ]:
1374639-74-3

[ Name ]:
Gemigliptin tartrate

Biological Activity

[Description]:

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[1][2].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Dipeptidyl Peptidase
Research Areas >> Metabolic Disease

[Target]

IC50: 10.3 nM (human recombinant DPP-4)[2]


[In Vitro]

Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1]. Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM[1]. Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Ki of 7.25 nM[2].

[In Vivo]

Gemigliptin tartrate (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo[1]. Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys[2]. Animal Model: Male C57BL/KsJ-db/db mice (7 weeks old)[1] Dosage: 100 mg/kg Administration: Oral gavage, daily, for 12 weeks Result: Significantly reduced circulating AGE levels by 44.5% in serum.

[References]

[1]. Jung E, et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo. Eur J Pharmacol. 2014 Dec 5;744:98-102.

[2]. Kim SH, et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo. Eur J Pharmacol. 2016 Oct 5;788:54-64.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H25F8N5O8

[ Molecular Weight ]:
639.45

Related Compounds