| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Alogliptin (formerly also known as SYR-322; trade names Nesina; Kazano, Oseni) is a novel, potent, orally bioavailable, and selective inhibitor of DPP-4 (serine protease dipeptidyl peptidase IV) that may have hypoglycemic effects. It shows >10,000-fold selectivity for inhibiting DPP-4 over the closely related DPP isoforms, like 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. Alogliptin does not lower the risk of heart attack or stroke, similar to other drugs used to treat Type 2 diabetes.
| Targets |
DPP-4 (IC50 = 2.93 nM)
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|---|---|
| ln Vitro |
Alogliptin shows more than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9 and is a potent (IC50 < 10 nM) inhibitor of DPP-4[1].Even at concentrations up to 30μM, compound 10 does not inhibit CYP-450 enzymes or block the hERG channel[2].
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| ln Vivo |
Analogliptin has an absolute oral bioavailability of 45%, 86%, and 72% to 88% in rats, dogs, and monkeys, respectively. Alogliptin administered orally results in plasma DPP-4 inhibition in rats, dogs, and monkeys within 15 minutes, with maximum inhibition exceeding 90%. The inhibition lasts for 12 hours in rats (43%), 6.5 hours in dogs, and 24 hours in monkeys (> 80%). Rats, dogs, and monkeys with mean alogliptin plasma concentrations (EC50) ranging from 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) exhibit 50% inhibition of DPP-4 activity, according to Emax modeling. Alogliptin, at doses of 0.3, 1, 3, and 10 mg/kg, inhibits plasma DPP-4 in Zucker fa/fa rats (91% to 100% at 2 hours and 20% to 66% at 24 hours), increases plasma GLP-1 (AUC0–20 min increases 2- to 3-fold), increases early-phase insulin secretion (AUC0–20 min increases 1.5–2.6 fold), and decreases blood glucose excursion (31%–67% decrease in AUC0–90 min) following oral glucose challenge. Normoglycemic rats' plasma glucose levels during fasting are unaffected by apelliptin (30 and 100 mg/kg).[3].
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| Enzyme Assay |
Alogliptin (also known as SYR-322) is a novel, potent, selective, and orally bioavailable inhibitor of DPP-4 (serine protease dipeptidyl peptidase IV). With an IC50 value of 2.6 nM, it shows over 10,000-fold selectivity for DPP-4 over DPP-8 and DPP-9, two closely related enzymes. Even at concentrations up to 30 μM, alogliptin does not block the hERG channel or inhibit CYP-450 enzyme activity.
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| Animal Protocol |
db/db mice
76.4 mg/kg/day oral |
| References |
| Molecular Formula |
C18H21N5O2
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|---|---|
| Molecular Weight |
339.39
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| Exact Mass |
339.17
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| Elemental Analysis |
C, 63.70; H, 6.24; N, 20.64; O, 9.43
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| CAS # |
850649-61-5
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| Related CAS # |
Alogliptin Benzoate;850649-62-6;Alogliptin-d3;1133421-35-8;Alogliptin-13C,d3 benzoate;Alogliptin-13C,d3;1246817-18-4
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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
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| InChi Key |
ZSBOMTDTBDDKMP-OAHLLOKOSA-N
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| InChi Code |
InChI=1S/C18H21N5O2/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/h2-3,5-6,9,15H,4,7-8,11-12,20H2,1H3/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
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| Synonyms |
SYR 322; Alogliptin; SYR-322; SYR322; Brand name: 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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30 mg/mL |
| Preparing Stock Solutions | 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 |
*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 |
| NCT01945242 | Completed | Drug: Alogliptin | Type 2 Diabetes Melitus | Takeda | March 2011 | |
| NCT03501277 | Completed | Drug: Alogliptin Drug: SYR-322-4833 BL |
Healthy Volunteers | Takeda | May 26, 2018 | Phase 1 |
| NCT01964963 | Completed | Drug: Alogliptin | Type 2 Diabetes Mellitus | Takeda | August 3, 2011 | |
| NCT02221284 | Completed | Drug: Alogliptin | Type 2 Diabetes Mellitus | Takeda | June 30, 2014 | |
| NCT03499704 | Active Recruiting |
Drug: Alogliptin Drug: Metformin |
Diabetes Mellitus, Type 2 | Celltrion Pharm, Inc. | February 11, 2020 | Phase 4 |
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