Date published: 2026-4-24

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Linagliptin (CAS 668270-12-0)

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Alternate Names:
Linagliptin is also known as BI-1356.
Application:
Linagliptin is a highly potent CD26 (DPP-4) inhibitor with over 10,000-fold selectivity over other peptidases and proteases.
CAS Number:
668270-12-0
Molecular Weight:
472.54
Molecular Formula:
C25H28N8O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Linagliptin is a compound that is utilized in biochemical and physiological research, particularly in the study of dipeptidyl peptidase-4 (DPP-4) inhibitors. As an inhibitor of the DPP-4 enzyme, Linagliptin is of interest in understanding the regulation of incretin hormones, which play a significant role in glucose homeostasis. Research involving Linagliptin includes investigations into its effects on glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP), which are hormones that influence insulin release and are degraded by DPP-4. Linagliptin is also used in studies examining its long-term impact on pancreatic beta cells and its potential effects on the cardiovascular system. Additionally, research into the molecular structure of Linagliptin and its binding interactions with DPP-4 contributes to the design of related compounds with improved efficacy and safety profiles. This research is for providing insights into metabolic regulation and the mechanisms that control blood sugar levels.


Linagliptin (CAS 668270-12-0) References

  1. (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.  |  Thomas, L., et al. 2008. J Pharmacol Exp Ther. 325: 175-82. PMID: 18223196
  2. Linagliptin: the newest dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus.  |  Aletti, R. and Cheng-Lai, A. 2012. Cardiol Rev. 20: 45-51. PMID: 22143285
  3. Linagliptin: a novel methylxanthin based approved dipeptidyl peptidase-4 inhibitor.  |  Agrawal, R., et al. 2012. Curr Drug Targets. 13: 970-83. PMID: 22420306
  4. SGLT2 Inhibitor Empagliflozin and DPP4 Inhibitor Linagliptin Reactivate Glomerular Autophagy in db/db Mice, a Model of Type 2 Diabetes.  |  Korbut, AI., et al. 2020. Int J Mol Sci. 21: PMID: 32340263
  5. Linagliptin, when compared to placebo, improves CD34+ve endothelial progenitor cells in type 2 diabetes subjects with chronic kidney disease taking metformin and/or insulin: a randomized controlled trial.  |  Awal, HB., et al. 2020. Cardiovasc Diabetol. 19: 72. PMID: 32493344
  6. Linagliptin prevents left ventricular stiffening by reducing titin cleavage and hypophosphorylation.  |  Cuijpers, I., et al. 2021. J Cell Mol Med. 25: 729-741. PMID: 33295687
  7. Linagliptin ameliorates pulmonary fibrosis in systemic sclerosis mouse model via inhibition of endothelial-to-mesenchymal transition.  |  Pei, B., et al. 2022. Mol Cell Biochem. 477: 995-1007. PMID: 34988855
  8. Linagliptin ameliorated interleukin-29-induced reduction of extracellular matrix genes through the nuclear factor erythroid 2-related factor 2 (Nrf2)/sry-type high-mobility-group box (SOX)-9 axis in an in vitro study on C-28/I2 chondrocytes.  |  Li, Y., et al. 2022. Bioengineered. 13: 3775-3784. PMID: 35081865
  9. Linagliptin ameliorates acetic acid-induced colitis via modulating AMPK/SIRT1/PGC-1α and JAK2/STAT3 signaling pathway in rats.  |  El-Ghannam, MS., et al. 2022. Toxicol Appl Pharmacol. 438: 115906. PMID: 35122774
  10. Neuroprotective effects of linagliptin in a rotenone-induced rat model of Parkinson's disease.  |  Abhangi, KV. and Patel, JI. 2022. Indian J Pharmacol. 54: 46-50. PMID: 35343207
  11. Linagliptin, a Selective Dipeptidyl Peptidase-4 Inhibitor, Reduces Physical and Behavioral Effects of Morphine Withdrawal.  |  Listos, J., et al. 2022. Molecules. 27: PMID: 35458676
  12. Linagliptin in Combination With Metformin Ameliorates Diabetic Osteoporosis Through Modulating BMP-2 and Sclerostin in the High-Fat Diet Fed C57BL/6 Mice.  |  Nirwan, N. and Vohora, D. 2022. Front Endocrinol (Lausanne). 13: 944323. PMID: 35928902
  13. Linagliptin and Vitamin D3 Synergistically Rescue Testicular Steroidogenesis and Spermatogenesis in Cisplatin-Exposed Rats: The Crosstalk of Endoplasmic Reticulum Stress with NF-κB/iNOS Activation.  |  Elrashidy, RA., et al. 2022. Molecules. 27: PMID: 36364125

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Linagliptin, 5 mg

sc-364721
5 mg
$260.00

Linagliptin, 10 mg

sc-364721A
10 mg
$426.00