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Alogliptin is an orally bioavailable dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50 = 6.9 nM) that is selective for DPP-4 over DPP-2, DPP-8, DPP-9, prolyl endopeptidase, fibroblast activation protein (FAP), and tryptase (IC50s = >100,000 nM). It does not inhibit cytochrome P450 enzymes and does not block the human ether-a-go-go-related gene (hERG) channel when used at concentrations up to 30 µM. Alogliptin inhibits DPP-4 activity in vivo in rats, dogs, and cynomolgus monkeys (EC50s = 3.4, 4.9, and 5.6 ng/ml, respectively, in plasma). It increases plasma glucagon-like peptide-1 (GLP-1, Cay-24460) and insulin levels and decreases blood glucose levels during an oral glucose challenge in Zucker fa/fa rats when administered at a dose of 10 mg/kg. Alogliptin (2.8 mg/kg per day) decreases plasma DPP-4 activity and increases GLP-1 levels in diabetic ob/ob mice when administered for 29 days. Formulations containing alogliptin have been used as an adjunct treatment for type 2 diabetes mellitus.Formal Name: 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile, monobenzoate. CAS Number: 850649-62-6. Synonyms: SYR-322. Molecular Formula: C18H21N5O2 . C7H6O2. Formula Weight: 461.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 0.1 mg/ml, DMSO: 0.1 mg/ml, Ethanol: slightly soluble, PBS (pH 7.2): 10 mg/ml. lambdamax: 225, 273 nm. SMILES: O=C(N(C)C1=O)C=C(N2C[C@H](N)CCC2)N1CC3=CC=CC=C3C#N.O=C(O)C4=CC=CC=C4. 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. InChi Key: KEJICOXJTRHYAK-XFULWGLBSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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