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BI-1356 (Linagliptin) | DPP-IV/DPP-4 inhibitor

  • BI-1356 (Linagliptin) (.png)
  • BI-1356 (Linagliptin) (.jpg)
Catalog #:

Product Description

BI-1356 (Linagliptin) is a highly potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50 = 1 nM) for treatment of type II diabetes. [1] BI-1356 can increase incretin levels (GLP-1 and GIP), which increases insulin secretion and inhibits glucagon release, decreases gastric emptying, and decreases blood glucose levels. BI-1356 shows 10,000-fold more selectivity for DPP-4 against other protease/peptidases, including DPP-8, DPP-9, trypsin, plasmin, and thrombin.[2]

Technical information:

Chemical Formula:   C25H28N8O2
CAS #:   668270-12-0
Molecular Weight:   472.54
Purity:   > 98%
Appearance:   White
Chemical Name:   (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione
Solubility:   Up to 25 mM in DMSO
Synonyms:   BI-1356, BI1356, Linagliptin, Tradjenta, Trajenta

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


1. Eckhardt M, et al. 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem. 2007; 50(26):6450-3. Pubmed ID: 18052023
2. Thomas L, et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J Pharmacol Exp Ther. 2008; 325(1):175-82. Pubmed ID: 18223196

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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