Catalog No.S2868

Alogliptin 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.

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Alogliptin Chemical Structure

Alogliptin Chemical Structure
Molecular Weight: 339.39

Validation & Quality Control

Quality Control & MSDS

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Alogliptin is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Description Alogliptin 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]
IC50 <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(Only for Reference)

Kinase Assay: [1]

DPP-4 Assay Solutions of test compounds in varying concentrations (≤10 mM final concentration) are prepared in DMSO and then diluted into assay buffer comprising: 20 mM Tris, pH 7.4; 20 mM KCl and 0.1 mg/mL BSA. Human DPP-4 (0.1 nM final concentration) is added to the dilutions and pre-incubats for 10 minutes at ambient temperature before the reaction is initiated with A-P-7-amido-4-trifluoromethylcoumarin (AP-AFC; 10 μM final concentration). The total volume of the reaction mixture is 10-100 μL depending on assay formats used (384 or 96 well plates). The reaction is followed kinetically (excitation λ= 400 nm; emission λ= 505 nm) for 5 - 10 minutes or an end-point is measured after 10 minutes. Inhibition constants (IC50) are calculated from the enzyme progress curves using standard mathematical models.

Animal Study: [2]

Animal Models The N-STZ-1.5 rats
Formulation 0.5% methylcellulose
Dosages 0.1, 0.3, 1 or 3 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Feng J, et al. J Med Chem, 2007, 50(10), 2297-2300.

[2] Asakawa T, et al. Life Sci, 2009, 85(3-4), 122-126.

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02771093 Recruiting Type 2 Diabetes Mellitus Takeda July 2016 Phase 4
NCT02756832 Not yet recruiting Diabetes Mellitus Takeda May 2016 --
NCT02763007 Not yet recruiting Diabetes Mellitus, Type 2 Kun-Ho Yoon|Takeda|The Catholic University of Korea May 2016 Phase 4
NCT02508168 Completed Healthy Volunteers Takeda April 2016 Phase 1
NCT02231021 Recruiting Type 2 Diabetes Mellitus Kun-Ho Yoon|Takeda|The Catholic University of Korea September 2014 Phase 4

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Chemical Information

Download Alogliptin SDF
Molecular Weight (MW) 339.39


CAS No. 850649-61-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms SYR-322
Solubility (25°C) * In vitro DMSO 68 mg/mL (200.35 mM)
Water 2 mg/mL (5.89 mM)
Ethanol <1 mg/mL
In vivo 0.5% methylcellulose 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name Benzonitrile, 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-

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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