Gemigliptin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型强效、选择性、竞争性、口服活性 DPP4 抑制剂，具有治疗 2 型糖尿病的潜力。

A novel potent, selective, competitive and orally active DPP4 inhibitor with potential for the treatment of type 2 diabetes; exhibits potent anti-glycation properties in vitro and in vivo, also improves renal function and attenuates podocyte injury in mice with diabetic nephropathy.Diabetes Approved.

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.

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. 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.

LC15-0444 | LC150444 | LC 150444

Metabolic Enzyme/Protease

DPP

DPP

Metabolic Disease

Diabetes

911637-19-9

489.37

C18H19F8N5O2

>98% (HPLC)

DMSO : ≥ 122.5 mg/mL 250.33 mM

C1CC(CN(C1=O)CC(CC(=O)N2CCC3=C(C2)N=C(N=C3C(F)(F)F)C(F)(F)F)N)(F)F

(S)-1-(2-amino-4-(2,4-bis(trifluoromethyl)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)-4-oxobutyl)-5,5-difluoropiperidin-2-one

(-20℃)

With Ice Pack

≥ 2 years