| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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Purity: ≥98%
Alogliptin benzoate (SYR-322 benzoate; Nesina; Kazano, Oseni), the benzoate salt of alogliptin, is a novel, potent, orally bioavailable, and selective inhibitor of DPP-4 (serine protease dipeptidyl peptidase IV), which has been shown to have anti-diabetic properties. It shows more than 10,000-fold selectivity for DPP-4 over the closely related DPP-8 and DPP-9, and inhibits DPP-4 with an IC50 value of 2.6 nM. This anti-diabetic medication has been sold in Japan since 2010. In 2013, the FDA approved the medication in three different forms: Nesina when taken alone, Kazano when taken with metformin, and Oseni when taken with pioglitazone. Anlogliptin does not lower the risk of heart attack or stroke, similar to other drugs used to treat Type 2 diabetes. When metformin alone is not sufficient to control a patient's diabetes, other gliptins such as alogliptin are frequently used in addition to the medication.
| Targets |
DPP-4 (IC50 <10 nM)
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|---|---|
| ln Vitro |
Alogliptin(SYR-322) is a potent inhibitor of DPP-4 and has selectivity over the closely related serine proteases DPP-8 and DPP-9 that is greater than 10,000 times. Even at concentrations up to 30 μM, alogliptin does not block the hERG channel or inhibit CYP-450 enzyme activity. [1]
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| ln Vivo |
Alogliptin (SYR-322) raises plasma insulin levels in female Wistar fatty rats and improves glucose tolerance in a dose-dependent manner.[1] When alogliptin is administered acutely, plasma active GLP-1 is increased and plasma DPP-4 activity is significantly decreased. At doses of 0.3 mg/kg and above, alogliptin improves glucose tolerance.It also increases plasma IRI in a dose-dependent manner, indicating that alogliptin's capacity to boost insulin secretion is the reason for the improved glucose tolerance.[2]
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| Enzyme Assay |
Alogliptin benzoate(SYR 322) is a potent, selective DPP-4 inhibitor with an IC50 of less than 10 nM. Its selectivity over DPP-8 and DPP-9 is more than 10,000 times superior.
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| Animal Protocol |
The N-STZ-1.5 rats
0.1, 0.3, 1 or 3 mg/kg p.o. |
| References |
| Molecular Formula |
C25H27N5O4
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|---|---|
| Molecular Weight |
461.51
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| Elemental Analysis |
C, 65.06; H, 5.90; N, 15.17; O, 13.87
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| CAS # |
850649-62-6
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| Related CAS # |
Alogliptin;850649-61-5;Alogliptin-13C,d3 benzoate
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| Appearance |
Solid powder
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| SMILES |
CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCC[C@H](C3)N.C1=CC=C(C=C1)C(=O)O
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| InChi Key |
KEJICOXJTRHYAK-XFULWGLBSA-N
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| InChi Code |
InChI=1S/C18H21N5O2.C7H6O2/c1-21-17(24)9-16(22-8-4-7-15(20)12-22)23(18(21)25)11-14-6-3-2-5-13(14)10-19;8-7(9)6-4-2-1-3-5-6/h2-3,5-6,9,15H,4,7-8,11-12,20H2,1H3;1-5H,(H,8,9)/t15-;/m1./s1
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| Chemical Name |
2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile;benzoic acid
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| Synonyms |
SYR-322 benzoate; SYR322; SYR 322; Alogliptin benzoate; Nesina; Kazano; Oseni
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
0.5% methylcellulose: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1668 mL | 10.8340 mL | 21.6680 mL | |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3336 mL | |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02756832 | Completed | Drug: Alogliptin Benzoate | Diabetes Mellitus | Takeda | September 20, 2016 | |
| NCT04980040 | Completed | Drug: Alogliptin Benzoate | Type 2 Diabetes Mellitus | Takeda | April 19, 2014 | |
| NCT02856113 | Completed | Drug: Alogliptin Benzoate Drug: Placebo |
Diabetes Mellitus, Type 2 | Takeda | October 14, 2016 | Phase 3 |
| NCT01990300 | Completed | Drug: Alogliptin/Pioglitazone | Type 2 Diabetes Mellitus | Takeda | November 28, 2011 | |
| NCT02798172 | Completed | Drug: Alogliptin and Metformin | Diabetes Mellitus, Type 2 | Fourth People's Hospital of Shenyang |
May 2014 | Not Applicable |
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