A potent DPP-4 inhibitor (IC50 = 1 nM for human recombinant DPP-4); ≥10

Linagliptin – 500 mg

Brand:
Cayman
CAS:
668270-12-0
Storage:
-20
UN-No:
Non-Hazardous - /

Linagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4) with an IC50 value of 1 nM for human recombinant DPP-4.{41123} It is selective, with ≥10,000-fold selectivity for DPP-4 over a panel of 11 peptidases and proteases. Linagliptin (3 mg/kg) inhibits 90% of plasma DPP-4 activity in rat. It also dose-dependently decreases plasma glucose and increases plasma levels of glucagon-like peptide 1 (GLP-1) and insulin in Zucker diabetic fatty rats. Oral administration of linagliptin reduces HbA1c levels in mice with high-fat diet- and low-dose streptozotocin-induced diabetes.{41124} Formulations containing linagliptin have been used for the treatment of type 2 diabetes mellitus.{41125}  

 

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Description

A potent DPP-4 inhibitor (IC50 = 1 nM for human recombinant DPP-4); ≥10,000-fold selectivity for DPP-4 over other a panel of 11 peptidases and proteases; inhibits 90% of plasma DPP-4 activity in rat; dose-dependently decreases plasma glucose and increases plasma levels of GLP-1 and insulin in Zucker diabetic fatty rats; reduces HbA1c levels in mice with high-fat diet- and low-dose streptozotocin-induced diabetes

Formal name: 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione

Synonyms:  BI-1356

Molecular weight: 472.5

CAS: 668270-12-0

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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