Catalog number: 850649-62-6
Category: Inhibitor
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Molecular Weight:
Alogliptin benzoate(SYR 322) 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.
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1.Characterization of process-related impurities including forced degradation products of alogliptin benzoate and the development of the corres
Zhou Y1, Zhou W, Sun L, Zou Q, Wei P, OuYang P. J Sep Sci. 2014 Jun;37(11):1248-55. doi: 10.1002/jssc.201301384. Epub 2014 Apr 25.
The characterization of process-related impurities and forced degradants of alogliptin benzoate (Alb) in bulk drugs and a stability-indicating HPLC method for the separation and quantification of all the impurities were investigated. Alb was found to be unstable under acid and alkali stress conditions and two major degradation products (Imp-F and Imp-G) were observed. The optimum separation was achieved on Kromasil C18 (250 × 4.6 mm, 5 μm) using 0.1% perchloric acid (pH adjusted to 3.0 with triethylamine) and acetonitrile as a mobile phase in gradient mode. The proposed method was found to be stability indicating, precise, linear (0.10-75.0 μg/mL), accurate, sensitive, and robust for the quantitation of Alb and its process-related substances and degradation products. The structures of 11 impurities were characterized and confirmed by NMR spectroscopy, MS, and IR spectroscopy, and the most probable formation mechanisms of all impurities were proposed according to the synthesis route.
2.Alogliptin benzoate for the treatment of type 2 diabetes.
Seino Y1, Yabe D. Expert Opin Pharmacother. 2014 Apr;15(6):851-63. doi: 10.1517/14656566.2014.898750.
INTRODUCTION: Type 2 diabetes mellitus continues to be a global problem, placing an enormous burden on healthcare systems and resources. Effective treatment options to minimize the effects of hyperglycemia are essential. Most patients eventually need to take multiple drugs to maintain glycemic control, and many antidiabetic drugs are associated with adverse effects, such as hypoglycemia, weight gain or gastrointestinal effects. Dipeptidyl peptidase (DPP)-4 inhibitor is one of the newer classes of oral antidiabetic drug, and alogliptin is the most recently approved drug in this class.
3.Alogliptin, a dipeptidylpeptidase-4 inhibitor, for patients with diabetes mellitus type 2, induces tolerance to focal cerebral ischemia in non-diabetic, normal mice.
Yang D1, Nakajo Y, Iihara K, Kataoka H, Yanamoto H. Brain Res. 2013 Jun 23;1517:104-13. doi: 10.1016/j.brainres.2013.04.015. Epub 2013 Apr 17.
Effective interventions that provide obvious neuroprotection are currently fairly limited. Glucagon-like peptide-1 (GLP-1), an enhancer of insulin production with a trophic effect on β cells in the islets, has been found to be trophic for neuronal cells. Alogliptin benzoate (AGL), a selective inhibitor of dipeptidylpeptidase-4 (DPP-4) functioning as a long-acting agonist of GLP-1, is in clinical use worldwide for patients with diabetes mellitus type 2. To clarify whether administration of AGL, independent of the insulinotropic effect, protects the brain against focal ischemia, we investigated the effect of AGL on the development of cerebral infarction in non-diabetic normal mice. Male C57BL/6J mice were administered AGL (7.5, 15, or 30μg) once a day for three weeks by intragastric gavage. After the induction of temporary focal ischemia, volumes of infarcted lesions and neurological deficits were analyzed at 24h (acute phase) and seven days (chronic phase).
4.Long-term effects of alogliptin benzoate in hemodialysis patients with diabetes: a 2-year study.
Nakamura Y1, Inagaki M, Shimizu T, Fujita K, Inoue M, Gotoh H, Oguchi K, Goto Y. Nephron Clin Pract. 2013;123(1-2):46-51. doi: 10.1159/000351678. Epub 2013 Jun 11.
AIM: To evaluate the long-term efficacy of monotherapy with the dipeptidase-4 inhibitor alogliptin benzoate in hemodialysis (HD) patients with type 2 diabetes.
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