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Gemigliptin Tartrate(911637-19-9 free base)

Catalog No. T7369L CAS 1374639-74-3

Synonyms: LC15-0444 tartrate

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.

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Gemigliptin Tartrate(911637-19-9 free base), CAS 1374639-74-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.
Targets&IC50	human recombinant DPP-4:10.3 nM
In vitro	Gemigliptin tartrate inhibits the formation of AGE-BSA with IC50 of 11.69 mM[1]. Gemigliptin tartrate 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 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].

Synonyms	LC15-0444 tartrate
Molecular Weight	639.45
Formula	C22H25F8N5O8
CAS No.	1374639-74-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 90mg/ml(140.75mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Jung E , Kim J , Kim S H , et al. Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivo.[J]. European Journal of Pharmacology, 2014, 744:98-102. 2. Kim S H , Jung E , Yoon M K , et al. Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivo[J]. European Journal of Pharmacology, 2016, 788:54-64.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gemigliptin Tartrate(911637-19-9 free base) 1374639-74-3 Proteases/Proteasome Ubiquitination DPP-4 Proteasome type Gemigliptin products mellitus peptidase-4 Gemigliptin Tartrate(911637 19 9 free base) dipeptidyl Gemigliptin Tartrate(911637199 free base) advanced diabetes LC15-0444 tartrate Inhibitor end glycation DPP Dipeptidyl Peptidase LC15-0444 AGE inhibit inhibitor

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