Gemigliptintartrate(LC15-0444tartrate)是一种高度选择性的，可逆的，竞争性的二肽基肽酶4(DPP-4)抑制剂，对人重组DPP-4作用的IC50值为10.3nM。Gemigliptintartrate具有很强的抗糖基化特性。Gemigliptintartrate可用于晚期糖基化终产物(AGE)相关的糖尿病并发症的研究。
货号:ajcx30710
CAS:1374639-74-3
分子式:C22H25F8N5O8
分子量：639.45
溶解度:DMSO: 100 mg/mL (156.38 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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]

[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.