Bulk Inquiry
Linagliptin
- BI 1356
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C25H28N8O2
- MW: 472.54
Description
Linagliptin (BI 1356) is a competitive and highly selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an in vitro IC50 value of approximately 1 nM. It is at least 10,000-fold selective for DPP-4 over DPP-8, DPP-9 and multiple related proteases and produces long-lasting enhancement of incretin signaling.
DPP-4 degrades incretin hormones such as GLP-1 and GIP, thereby influencing glucose-dependent insulin secretion. Linagliptin is a reference compound for DPP-4 pharmacology and type 2 diabetes-related incretin research.
Key Features
- Highly potent DPP-4 inhibitor
- IC50: approximately 1 nM
- ≥10,000-fold selectivity over DPP-8 and DPP-9
- Enhances incretin-dependent glucose regulation
Applications
- DPP-4 enzyme pharmacology
- Incretin signaling studies
- Type 2 diabetes model research
- Glucose tolerance and insulin secretion assays
More Information
| Parent CAS No. | 668270-12-0 |
|---|---|
| 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 |
| SMILES | N1(CC#CC)C2=C(N(C)C(=O)N(CC3=NC(C)=C4C(=N3)C=CC=C4)C2=O)N=C1N1CCC[C@@H](N)C1 |&1:32,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1 |
| InChiKey | LTXREWYXXSTFRX-QGZVFWFLSA-N |
| CID | 10096344 |
| Short Description | DPP4 inhibitor |
References
- J. Rungby. Inhibition of dipeptidyl peptidase 4 by BI-1356, a new drug for the treatment of beta-cell failure in type 2 diabetes. Exp.Opin. Investig. Drugs. 2009, 18, 835-838.
- L. Thomas 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,…. J. Pharmacol. Exp. Ther. 2008, 325, 175-182.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 4464 | UAMC-1110 |
From $154.00 |
| 1228 | Butabindide oxalate |
From $115.50 |
| 1631 | Vildagliptin |
From $66.00 |
| 2434 | 1-Deazaadenosine |
From $154.00 |
| 2470 | Trelagliptin succinate |
From $159.50 |
| 2766 | AZD7986 |
From $154.00 |
| 3251 | Sitagliptin |
From $55.00 |
| 3309 | Teneligliptin hydrobromide |
From $55.00 |
| 3310 | Alogliptin benzoate |
From $71.50 |
| 3438 | NDMC101 |
From $99.00 |
