Alogliptin (SYR-322) |
| Catalog No.GC15130 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 850649-61-5
Sample solution is provided at 25 µL, 10mM.
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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
[1].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
| Cell experiment: [1] | |
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Cell lines |
U937 histiocyte |
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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. |
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Reaction Conditions |
5 nM, 48h, inhibited cell proliferation 1 nM, 48h, inhibited MMP-1 secretion |
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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] | |
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Animal models |
Zucker fa/fa rats |
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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. |
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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. |
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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. |
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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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| Cas No. | 850649-61-5 | SDF | |
| 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 | ≥ 14.75 mg/mL in DMSO, ≥ 100 mg/mL in EtOH with ultrasonic | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9465 mL | 14.7323 mL | 29.4646 mL |
| 5 mM | 0.5893 mL | 2.9465 mL | 5.8929 mL |
| 10 mM | 0.2946 mL | 1.4732 mL | 2.9465 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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