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.

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

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

[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 http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02231021 Not yet recruiting Type 2 Diabetes Mellitus Kun-Ho Yoon|Takeda|The Catholic University of Korea September 2014 Phase 4
NCT02221284 Recruiting Type 2 Diabetes Mellitus Takeda June 2014 --
NCT02068443 Recruiting Diabetes Takeda January 2014 Phase 3
NCT01890122 Recruiting Diabetes Mellitus Takeda September 2013 Phase 3
NCT01588587 Not yet recruiting Type 2 Diabetes Mellitus Nagaoka Red Cross Hospital|Kurume University October 2012 --

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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
Synonyms SYR-322
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]-

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Tech Support & FAQs

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