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Alogliptin Benzoate

Catalog No.
A3156
DPP-4 inhibitor,selective and potent,antidiabetic drug
Grouped product items
SizePriceStock Qty
5mg
$60.00
In stock
10mg
$100.00
In stock
50mg
$320.00
In stock
100mg
$470.00
In stock

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Email: [email protected]

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Background

Alogliptin is a novel, highly selective and potent inhibitor of serine protease dipeptidylpeptidase-4 (DPP-4) with IC50 value of less than 10 nM [1].

Alogliptin has been reported to significantly reduce plasma DPP-4 activity and increase active GLP-1 levels in a dose-dependent manner in ob/ob mice. Besides, alogliptin after 4 weeks administration remarkably reduced non-fasting glycosylated hemoglobin, non-fasting plasma glucose and triglyceride levels, as well as siginificantly increased non-fasting plasma insulin and fasting pancreatic insulin content in ob/ob mice. Moreover, alogliptin treated ob/ob mice have shown the increase of early-phase insulin secretion and the decrease of plasma glucose AUC [2]

References:
[1] Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB, Navre M, Shi L, Skene RJ, Asakawa T, Takeuchi K, Xu R, Webb DR, Gwaltney SL 2nd. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300.
[2] Moritoh Y1, Takeuchi K, Asakawa T, Kataoka O, Odaka H. Chronic administration of alogliptin, a novel, potent, and highly selective dipeptidyl peptidase-4 inhibitor, improves glycemic control and beta-cell function in obese diabetic ob/ob mice. Eur J Pharmacol. 2008 Jul 7;588(2-3):325-32.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt461.51
Cas No.850649-62-6
FormulaC25H27N5O4
SynonymsSYR322, SYR-322,Nesina;
Solubility≥46.2 mg/mL in DMSO, ≥3.02 mg/mL in EtOH with ultrasonic and warming, ≥46.2 mg/mL in H2O with gentle warming
Chemical Name2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile;benzoic acid
SDFDownload SDF
Canonical SMILESCN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N.C1=CC=C(C=C1)C(=O)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Alogliptin benzoate(SYR 322) is a potent, selective inhibitor of DPP-4 with an IC50 value of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.
Targets DPP-4          
IC50 <10 nM          

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