(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
CAS:668270-12-0
Chemical Formula:C25H28N8O2
MW:472.54
Availability: R&D; Commercialization
⬤ CAS No.668270-12-0
⬤ Packaging type：
20kg barrel；5kg barrel；1kg bag；500g bag ; Customized Packaging
| English Name | Linagliptin |
| CAS No. | 668270-12-0 |
| Chemical Formula | C25H28N8O2 |
| Molecular Weight | 472.54 |
| EINECS | 1308068-626-2 |
| Related Categories | Pharmaceutical intermediates, pharmaceutical raw materials, fine chemicals |
| Mol | 668270-12-0.mol |
| Melting point | 202 ºC |
| Boiling point | 661.2±65.0 °C (Predicted) |
| Density | 1.39 |
| Storage conditions | Refrigerator |
| Solubility | Soluble in chloroform (a small amount), DMSO (a small amount), methanol (a small amount) |
| Acidity coefficient (pKa) | 10.01±0.20 (Predicted) |
| Form | Solid |
| Color | White to orange |
| Side Effects | Hypoglycemia, gastrointestinal discomfort (nausea, vomiting, diarrhea), allergic reactions (skin rash, itching), joint pain |
| Precautions | Not for use in patients with type 1 diabetes or diabetic ketoacidosis. Use with caution in patients with severe liver or kidney disease. Safety in pregnant and lactating women is not established. |
| Drug Interactions | Potential interactions with other antidiabetic medications. Consult healthcare provider before use. |
| Contraindications | Hypersensitivity to linagliptin or any of its components. |
| Uses | Lilagliptin is a new type of highly effective and selective dipeptidyl peptide-4 (DPP-4) inhibitor for the treatment of type 2 diabetes. |
| Mechanism of Action | Lilagliptin is a DPP-IV inhibitor. DPP-IV is an incretin hormone that exists in many tissues bound to proteins, such as the kidney, liver, brush edge of the small intestinal membrane, pancreatic duct, lymphocytes, endothelial cells, etc. The enzyme can inactivate GLP-1 by hydrolyzing the second alanine at the N-terminus. Therefore, inhibiting the enzyme can increase the concentration of GLP-1, prompting pancreatic cells to produce insulin, while reducing the concentration of glucagon, thereby exerting an anti-diabetic effect. |
| Side Effects | The most common side effects of linagliptin include upper respiratory tract infection, nasal congestion or runny nose, sore throat, muscle pain, headache, etc., and its mechanism needs further study. |
| Biological Activity | Linagliptin (BI-1356) is a highly potent and selective DPP-4 inhibitor with an IC50 of 1nM. It is more than 10,000-fold more selective for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP9. Linagliptin activates glomerular autophagy in a type 2 diabetes model. DPP4 mediates ferroptosis in TP53-deficient CRC cells. |
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