Gemigliptin Tartrate(911637-19-9 free base)

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

Gemigliptin tartrate 是一种高选择性、可逆、竞争性的二肽基肽酶 4 (DPP-4) 抑制剂。

Gemigliptin tartrate is a highly selective, reversible and competitive inhibitor of dipeptidyl peptidase-4 (DPP-4). It has an?IC50?of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties.

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.

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. 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 tartrate

Metabolic Enzyme/Protease

DPP

DPP-4

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1374639-74-3

639.45

C22H25F8N5O8

>98% (HPLC)

DMSO:90mg/ml(140.75mM; need ultrasonic)

O=C([C@@H]([C@H](C(O)=O)O)O)O.O=C1N(CC(F)(CC1)F)C[C@H](CC(N2CCC3=C(N=C(N=C3C2)C(F)(F)F)C(F)(F)F)=O)N

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(-20℃)

With Ice Pack

≥ 2 years