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Alogliptin (SYR-322)
DPP-4 inhibitor,potent and highly selective

Alogliptin (SYR-322)

Catalog No. A4038
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $100.00 In stock
10mg $140.00 In stock
50mg $560.00 In stock
100mg $920.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Alogliptin (SYR-322)

Related Biological Data

Alogliptin (SYR-322)

Related Biological Data

Alogliptin (SYR-322)

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          
IC50 < 10 nM          

Protocol

Cell experiment: [1]

Cell lines

U937 histiocyte

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

5 nM, 48h, inhibited cell proliferation 1 nM, 48h, inhibited MMP-1 secretion

Applications

Alogliptin inhibited cell proliferation by 53% at concentration of 5 nM. At 1 nM, alogliptin inhibited MMP-1 secretion significantly, suggesting that the inhibitory effect of alogliptin on MMP is not associated with that on cell proliferation.

Animal experiment : [2]

Animal models

Zucker fa/fa rats

Dosage form

Eight-week-old male Zucker fa/fa rats were divided into 5 groups based on body weight and fasting plasma glucose levels and administered vehicle alone (0.5% carboxymethylcellulose) or alogliptin at 0.3, 1, 3, or 10 mg/kg by single bolus oral gavage (5 ml/kg dose volume). At 30 min postdose, rats were given a glucose solution (1 g/kg, 2ml/kg dose volume). Blood glucose concentrations were analyzed up to 90min after glucose load using the Accu-Chek glucometer and plasma insulin concentrations were analyzed up to 60 min after glucose load using an insulin ELISA kit.

Applications

Early-phase insulin secretion was increased after a single dose of alogliptin compared with vehicle alone. Alogliptin increased about 1.5, 1.5, and 1.8 fold for the 0.3, 1, and 3 mg/kg doses. Significant decreases in blood glucose excursion were observed for all alogliptin doses compared with vehicle alone after an oral glucose load. Mean baseline-adjusted blood glucose AUC0–90 min was decreased by approximately 31%, 37%, and 41% for the 0.3, 1, and 3 mg/kg doses, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Ta N N, Li Y, Schuyler C A, et al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis, 2010, 213(2): 429-435.

[2] Lee B, Shi L, Kassel D B, et al. Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. European journal of pharmacology, 2008, 589(1): 306-314.

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Chemical Properties

Cas No. 850649-61-5 SDF Download SDF
Synonyms Alogliptin,SYR322
Chemical Name 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile
Canonical SMILES CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N
Formula C18H21N5O2 M.Wt 339.39
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips No
Shipping Condition No

View Related Products By Research Topics

Research Update

1. Alogliptin: Safety, Efficacy, and Clinical Implications. J Pharm Pract. 2014 Feb 13. [Epub ahead of print]
Abstract
Alogliptin is not only an inhibitor of DPP-4 that raises postprandial levels of glucagon-like peptide 1 resulting in insulin secretion and glucose homeostasis but also a safe and tolerable anti-diabetic agent showing a significant reduction in HdA1c when used alone or with other anti-diabetic agents.
2. Alogliptin: a new dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus. Ann Pharmacother. 2013 Nov;47(11):1532-9. doi: 10.1177/1060028013504076.
Abstract
Alogliptin, a DPP-4 inhibitor, has been reviewed for its pharmacology, pharmacokinetics, safety and efficacy in the managment of T2DM.
3. Cardiovascular safety of the dipetidyl peptidase-4 inhibitor alogliptin in type 2 diabetes mellitus. Diabetes Obes Metab. 2013 Jul;15(7):668-73. doi: 10.1111/dom.12093. Epub 2013 Apr 4.
Abstract
The cardiovascular profile of alogliptin, a DPP-4 inhibitor, has been evaluated due to increased CV risk associated with the treatment of type 2 diabetes.
4. Alogliptin after acute coronary syndrome in patients with type 2 diabetes. N Engl J Med. 2013 Oct 3;369(14):1327-35. doi: 10.1056/NEJMoa1305889. Epub 2013 Sep 2.
Abstract
Alogliptin, a DPP-4 inhibitor, has been assessed for its cardiovascular outcomes in patients with type 2 diabetes and a recent acute coronary syndrome.

Background

Alogliptin (also known as SYR-322), is a novel, orally-available and highly selective quinazolinone-based inhibitor of dipeptidyl peptidase-4 (DPP-4), a serine aminopeptidase catalyzing the cleavage of peptides, that potently inhibits human DPP-4 in vitro with 50% inhibition concentration IC50 value of 6.9 nM and barely exhibits any inhibition towards the closely related serine proteases, including DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidas and tryptase (IC50 > 100,000 nM for all). Alogliptin prevents DPP-4-catalyzed degradation of GLP-1 and GIP, which regulate concentrations of blood glucose by stimulating glucose-dependent insulin secretion, and hence is being investigated in the treatment of type 2 diabetes.

Reference

Bumsup Lee, Lihong Shi, Daniel B. Kassel, Tomoko Asakawa, Koji Takeuchi and Ronald J. Christopher. Pharmacokinetic, pharmacodynamics, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. European Journal of Pharmacology 589 (2008) 306-314