D3572
Dipeptidyl Peptidase IV Inhibitor IV
Synonym(s):
(S)-1-(4-Methyl-1-(2-pyrimidinyl)-4-piperidylamino)acetyl-2-pyrrolidinecarbonitrile, K579
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About This Item
Empirical Formula (Hill Notation):
C17H24N6O
Molecular Weight:
328.41
UNSPSC Code:
12352202
NACRES:
NA.77
General description
Dipeptidyl Peptidase IV Inhibitor IV, also known as K579 ((S)-1-[4-methyl-1-(2-pyrimidinyl)-4-piperidylamino]acetyl-2-pyrrolidinecarbonitrile), is orally available. It has a formula weight of 339.39 g/mol.
Biochem/physiol Actions
Dipeptidyl peptidase IV (DPP IV) is a key enzyme involved in the regulation of incretin hormone levels in the gastrointestinal tract. Incretin hormones, such as glucagon like peptide (GLP-1) and glucose-dependent insulinotropic hormone (GIP) / gastric inhibitory peptide, cause the glucose stimulated release of insulin. This allows the endocrine system to preemptively stimulate release insulin in response to ingestion of high sugar foods. Type 2 diabetics demonstrate a greatly reduced incretin induced insulin release response.
This response in hyperglycemic conditions is counterbalanced by the rapid rate of degradation of these incretin hormones by dipeptidyl peptidase IV in normal conditions. Inhibition of dipeptidyl peptidase IV results in longer lifetime of the incretin hormones in the GI tract and thus prolonged stimulation of insulin production. Specific dipeptidyl peptidase inhibitors are actively being explored as drug targets for treating type 2 diabetes and several candidates are actively in clinical trial.
This response in hyperglycemic conditions is counterbalanced by the rapid rate of degradation of these incretin hormones by dipeptidyl peptidase IV in normal conditions. Inhibition of dipeptidyl peptidase IV results in longer lifetime of the incretin hormones in the GI tract and thus prolonged stimulation of insulin production. Specific dipeptidyl peptidase inhibitors are actively being explored as drug targets for treating type 2 diabetes and several candidates are actively in clinical trial.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
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A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads.
Purich D.
The Inhibitor Index (2017)
Involvement of the active metabolites in the inhibitory activity of K579 on rat plasma dipeptidyl peptidase IV.
Takasaki K, et al.
European Journal of Pharmacology, 505(1-3), 237-241 (2004)
Loss of incretin effect is a specific, important, and early characteristic of type 2 diabetes.
Holst J J, et al.
Diabetes Care, 34(2), S251-S257 (2011)
Dipeptidyl peptidase IV (DPP IV) inhibitors: a newly emerging drug class for the treatment of type 2 diabetes.
Green BD, et al.
Diabetes & Vascular Disease Research : Official Journal of the International Society of Diabetes and Vascular Disease, 3(3), 159-165 (2006)
Ying Wang et al.
Acta pharmaceutica Sinica. B, 11(6), 1568-1577 (2021-07-06)
IF1 (ATPIF1) is a nuclear DNA-encoded mitochondrial protein whose activity is inhibition of the F1Fo-ATP synthase to control ATP production. IF1 activity remains unknown in the regulation of GLP-1 activity. In this study, IF1 was examined in the diet-induced obese
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