An orally bioavailable DPP-4 inhibitor (IC50 = 6.9 nM) that is selective for DPP-4 over DPP-2

Alogliptin (benzoate salt) – 25 mg

Brand:
Cayman
CAS:
850649-62-6
Storage:
-20
UN-No:
Non-Hazardous - /

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).{36524} 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.{36525} 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).{36524} It increases plasma glucagon-like peptide-1 (GLP-1; Item No. 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.{36526} Formulations containing alogliptin have been used as an adjunct treatment for type 2 diabetes mellitus.  

 

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Description

An orally bioavailable DPP-4 inhibitor (IC50 = 6.9 nM) that is selective for DPP-4 over DPP-2, DPP-8, DPP-9, prolyl endopeptidase, FAP, and tryptase (IC50s = >100,000 nM); 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); increases plasma GLP-1 and insulin levels and decreases blood glucose levels during an oral glucose challenge in Zucker fa/fa rats (10 mg/kg); decreases plasma DPP-4 activity and increases GLP-1 levels in diabetic ob/ob mice when administered for 29 days (2.8 mg/kg per day)

Formal name: 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile, monobenzoate

Synonyms:  SYR-322

Molecular weight: 461.5

CAS: 850649-62-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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