Alogliptin

Catalog No.S2868 Synonyms: SYR-322

Alogliptin Chemical Structure

Molecular Weight(MW): 339.39

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.

Size Price Stock Quantity  
In DMSO USD 370 In stock
USD 270 In stock
USD 470 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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]
<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]
+ Expand
  • 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.
    (Only for Reference)

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 Information

Molecular Weight 339.39
Formula

C18H21N5O2

CAS No. 850649-61-5
Storage powder
in solvent
Synonyms SYR-322

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03042325 Not yet recruiting Diabetes Mellitus, Type 2 Takeda March 2017 Phase 4
NCT02989649 Recruiting Diabetes Mellitus, Type 2 Takeda December 2016 --
NCT02856113 Recruiting Diabetes Mellitus, Type 2 Takeda November 2016 Phase 3
NCT02756832 Recruiting Diabetes Mellitus Takeda September 2016 Phase 4
NCT02771093 Recruiting Type 2 Diabetes Mellitus Takeda July 2016 Phase 4
NCT02763007 Not yet recruiting Diabetes Mellitus, Type 2 Kun-Ho Yoon|Takeda|The Catholic University of Korea May 2016 Phase 4

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID