Alogliptin

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. Phase 4.

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In DMSO USD 370 In stock
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Alogliptin Chemical Structure

Alogliptin Chemical Structure
Molecular Weight: 339.39

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

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. Phase 4.
Targets DPP-4
IC50 < 10 nM [1]
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]
Features

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
Dosages 0.1, 0.3, 1 or 3 mg/kg
Administration p.o.
Solubility 0.5% methylcellulose, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01521962 Recruiting Diabetes Mellitus Takeda|Takeda Pharmaceutical Company Limited 2012-02 Phase 3
NCT01632007 Recruiting Diabetes Mellitus Takeda|Takeda Pharmaceutical Company Limited 2012-05 Phase 3
NCT01664624 Completed Type 2 Diabetes Takeda 2012-07 Phase 1
NCT01686711 Recruiting Diabetes Mellitus Takeda|Takeda Pharmaceutical Company Limited 2012-09 Phase 4
NCT01588587 Not yet recruiting Type 2 Diabetes Mellitus Nagaoka Red Cross Hospital|Kurume University 2012-10

Chemical Information

Download Alogliptin SDF
Molecular Weight (MW) 339.39
Formula

C18H21N5O2

CAS No. 850649-61-5
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 68 mg/mL (200 mM)
Water 2 mg/mL (5 mM)
Ethanol <1 mg/mL (<1 mM)
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]-

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.33939 3.3939 6.7878 10.1817

Research Area

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