Home Proteases DPP-4 inhibitor Alogliptin

Alogliptin

Catalog No.S5365 Synonyms: SYR 322

For research use only.

Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.

Alogliptin Chemical Structure

CAS No. 850649-61-5

Selleck's Alogliptin has been cited by 1 Publication

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Biological Activity

Description Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.
Targets
DPP-4 [1]
(293E cells lysates)
2.93 nM
In vitro

Alogliptin is a potent (IC50 < 10 nM) inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9[1].Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM[2].
In vivo Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats.[3].

Protocol (from reference)

Animal Research:

[4]
  • Animal Models: db/db mice
  • Dosages: 76.4 mg/kg/day
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 67 mg/mL
(197.41 mM)
Ethanol 67 mg/mL
(197.41 mM)
Water 18 mg/mL
(53.03 mM)

* 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 339.39
Formula

C18H21N5O2
CAS No. 850649-61-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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