ALOGLIPTIN(ALOGLIPTINE, ALOGLIPTINA) Chemical Properties

Melting point:

127 - 129°C

Boiling point:

519.2±60.0 °C(Predicted)

Density 

1.342

Flash point:

267.8℃

storage temp. 

Refrigerator

solubility 

Chloroform (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly)

form 

Solid

pka

9.89±0.20(Predicted)

color 

White to Off-White

Safety Information

Safety Statements 

24/25

RIDADR 

3077

HS Code 

29335990

Hazardous Substances Data

850649-61-5(Hazardous Substances Data)

ALOGLIPTIN(ALOGLIPTINE, ALOGLIPTINA) Usage And Synthesis

Description

Alogliptin is a dipeptidyl-peptidase IV (DPP-4) inhibitor that was approved in Japan in 2010 for treatment of type 2 diabetes, a disease in which insulin resistance and β-cell dysfunction lead to hyperglycemia. As islet function is lost, the severity of insulin resistance increases. The introduction of DPP-4 inhibitors has brought a novel class of insulinotropic agents for the treatment options available to type 2 diabetic patients. The therapeutic potential of glucagon-like peptide 1 (GLP-1), an incretin peptide, for the treatment of type 2 diabetes was realized in the 1990s. The insulinotropic effects of GLP-1 depend closely on glucose concentrations providing the possibility of glucose normalization without the risk of hypoglycemia. GLP-1 has other non-insulinotropic physiological actions that are advantageous. It suppresses glucagon secretion from a cells and slows gastric emptying, which contributes to satiety and to a slower passage and reabsorption of carbohydrates. GLP-1 also contributes to satiety via a central mechanism as a neurotransmitter with effects on the hypothalamus.

Chemical Properties

White Solid

Originator

Syrrx Inc. (now Takeda San Diego) (Japan)

Uses

Alogliptin is an oral antihyperglycemic agent that is a selective inhibitor of the enzyme dipeptidyl peptidase-4 (DPP-4). Antidiabetic agent.

Definition

ChEBI: A piperidine that is 3-methyl-2,4-dioxo-3,4-dihydropyrimidine carrying additional 2-cyanobenzyl and 3-aminopiperidin-1-yl groups at positions 1 and 2 respectively (the R-enantiomer). Used in the form of its benzoate salt for treatment of t pe 2 diabetes.

brand name

Nesina

Clinical Use

Dipeptidyl peptidase 4 inhibitor:
Treatment of type 2 diabetes in combination with other therapies

target

DPP-4

Metabolism

Alogliptin does not undergo extensive metabolism. Two minor metabolites were detected following administration of an oral dose of [14C]-alogliptin, N-demethylated alogliptin, M-I (<1% of the parent compound), and N-acetylated alogliptin, M-II (<6% of the parent compound). M-I is an active metabolite and is a highly selective inhibitor of DPP-4 similar to alogliptin; M-II does not display any inhibitory activity towards DPP-4 or other DPP-related enzymes. In vitro data indicate that CYP2D6 and CYP3A4 contribute to the limited metabolism of alogliptin.

ALOGLIPTIN(ALOGLIPTINE, ALOGLIPTINA)(850649-61-5)Related Product Information

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