Proteases (Di- and tripeptidyl)
Di- and tripeptidyl peptidases (EC 3.4.14.-) make up an individual class of aminopeptidases. DPP4 (EC 3.4.14.5) is also known as adenosine deaminase complexing protein 2 or CD26 (cluster of differentiation 26). It is an antigenic enzyme expressed on the surface of most cell types and is associated with immune regulation, signal transduction and apoptosis. It is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides. Additionally, it has been proven to be implicated in the pathogenesis of type 2 diabetes[1]. Butabindide oxalate (Axon 1228) has proven to inhibit the cholecystokinin-8 (CCK-8)-inactivating peptidase, which is in fact a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4.14.10). CCK-8 in its sulfated form functions as a neurotransmitter. It is released in response to ingestion of food and is involved in the control of food digestion through regulation of gallbladder contraction, pancreatic secretion, and contraction of the pyloric sphincter to delay gastric emptying. Inhibition of the enzyme therefore could be an opportunity to treat obesity related metabolic diseases[2].
[1] Vildagliptin, a dipetidyl peptidase-IV inhibitor, improves model-assessed β-cell function in patients with type 2 diabetes. A. Mari et al. J. Clin. Endocrinol. Metab. 2005, 90, 4888-4894.
[2] Inhibitors of Tripeptidyl Peptidase II. 3. Derivation of Butabindide by Successive Structure Optimizations Leading to a Potential General Approach to Designing Exopeptidase Inhibitors. C.R. Ganellin et al. J. Med. Chem., 2005, 48, 7333-7342.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3310 | Alogliptin benzoate | Potent, highly selective and orally active DPP-4 inhibitor | €65.00 | |
| 2766 | AZD7986 | Potent, reversible, and selective DPP1 inhibitor | €140.00 | |
| 1228 | Butabindide oxalate | TPP2 inhibitor | €110.00 | |
| 2354 | Linagliptin | Competitive and highly selective dipeptidyl peptidase (DPP)-4 inhibitor | €90.00 | |
| 3438 | NDMC101 | DPP-4 inhibitor; Osteoclastogenesis inhibitor | €90.00 | |
| 3492 | Perindopril erbumine | Orally bioavailable long-acting ACE inhibitor | €60.00 | |
| 3655 | Quinapril hydrochloride | ACE inhibitor | €50.00 | |
| 3251 | Sitagliptin | Potent, selective and orally active DPP-4 inhibitor | €50.00 | |
| 3309 | Teneligliptin hydrobromide | Highly potent, selective, long-lasting and orally active DPP-4 inhibitor | €50.00 | |
| 2470 | Trelagliptin succinate | Orally active DPP4 inhibitor for the treatment of type 2 diabetes | €145.00 | |
| 1631 | Vildagliptin | DPP4 inhibitor | €60.00 | |