Alogliptin (SYR-322) benzoate

For research use only.

Catalog No.S2868 Synonyms: SYR-322

1 publication

Alogliptin (SYR-322) benzoate Chemical Structure

CAS No. 850649-62-6

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.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 363 In stock
EUR 265 In stock
EUR 461 In stock
EUR 1641 In stock
EUR 2427 In stock
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Selleck's Alogliptin (SYR-322) benzoate has been cited by 1 publication

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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

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 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]

Protocol

Animal Research:[2]
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  • Animal Models: The N-STZ-1.5 rats
  • Dosages: 0.1, 0.3, 1 or 3 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 68 mg/mL (147.34 mM)
Water 2 mg/mL (4.33 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.51
Formula

C18H21N5O2.C7H6O2

CAS No. 850649-62-6
Storage powder
in solvent
Synonyms SYR-322
Smiles CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N.C1=CC=C(C=C1)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03501277 Completed Drug: Alogliptin|Drug: Pioglitazone|Drug: SYR-322-4833 BL Healthy Volunteers Takeda May 26 2018 Phase 1
NCT02276274 Completed Drug: SYR-322-MET Clinical Pharmacology Takeda June 2014 Phase 3
NCT00957268 Completed Drug: Alogliptin Diabetes Mellitus Type 2 Takeda September 2009 Phase 1

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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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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID