Home Proteases DPP inhibitor Alogliptin (SYR-322) benzoate For research use only.

Alogliptin (SYR-322) benzoate

Synonyms: SYR-322

Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.

Alogliptin (SYR-322) benzoate Chemical Structure

Alogliptin (SYR-322) benzoate Chemical Structure

CAS: 850649-62-6

Selleck's Alogliptin (SYR-322) benzoate has been cited by 1 publication

Purity & Quality Control

Batch: S286801 DMSO] 68 mg/mL] false] Water] 2 mg/mL] false] Ethanol] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.
Targets
DPP-4 [1]
<10 nM
In vitro
In vitro Alogliptin(SYR-322) is a potent inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. Alogliptin is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30 μM. [1]
In Vivo
In vivo Alogliptin(SYR-322) produces dose-dependent improvements in glucose tolerance and increases plasma insulin levels in female Wistar fatty rats. [1] Acute administration of alogliptin results in a significant decrease in plasma DPP-4 activity, and increases plasma active GLP-1. Alogliptin improves glucose tolerance at a dose of 0.3 mg/kg and higher, with a dose-dependent increase in plasma IRI, suggesting that improved glucose tolerance results from the ability of alogliptin to enhance insulin secretion. [2]
Animal Research Animal Models The N-STZ-1.5 rats
Dosages 0.1, 0.3, 1 or 3 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03501277 Completed Healthy Volunteers Takeda May 26 2018 Phase 1
NCT02276274 Completed Clinical Pharmacology Takeda June 2014 Phase 3
NCT00957268 Completed Diabetes Mellitus Type 2 Takeda September 2009 Phase 1

Chemical lnformation & Solubility

Molecular Weight 461.51 Formula

C18H21N5O2.C7H6O2
CAS No. 850649-62-6 SDF Download Alogliptin (SYR-322) benzoate SDF
Smiles CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N.C1=CC=C(C=C1)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 68 mg/mL ( (147.34 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble


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In vivo
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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