Linagliptin
- CAS No.
- 668270-12-0
- Chemical Name:
- Linagliptin
- Synonyms
- Linagliptin API;Linaglitpin;Linagliptin (BI-1356);8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione;inag;iptin;inagL;Ondero;CS-494;Bi 1356
- CBNumber:
- CB71518518
- Molecular Formula:
- C25H28N8O2
- Molecular Weight:
- 472.54
- MOL File:
- 668270-12-0.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/6/27 18:15:55
| Melting point | 202 ºC |
|---|---|
| Boiling point | 661.2±65.0 °C(Predicted) |
| Density | 1.39 |
| storage temp. | Refrigerator |
| solubility | Chloroform (Sparingly), DMSO (Slightly), Methanol (Slightly) |
| pka | 10.01±0.20(Predicted) |
| form | Solid |
| color | White to Orange |
| InChIKey | LTXREWYXXSTFRX-QGZVFWFLSA-N |
| 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 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H319-H335-H315 | |||||||||
| Precautionary statements | P264-P280-P305+P351+P338-P337+P313P-P264-P280-P302+P352-P321-P332+P313-P362 | |||||||||
| HS Code | 29335990 | |||||||||
| NFPA 704 |
|
Linagliptin Chemical Properties,Uses,Production
Description
Linagliptin (trade names Tradjenta and Trajetna) is an inhibitor of dipeptidyl peptidase-4 (DPP-4) that was approved by the U.S. FDA in May 2011 for the treatment of Type 2 diabetes along with diet and exercise. Linagliptin (BI-1356) has been described as a potent highly selective, slow-off rate and long acting inhibitor of DPP-4. Linagliptin arose from optimization efforts of xanthine-based DPP-4 inhibitors with the initial lead identified from an HTS campaign. After optimizing the activity of the initial micromolar lead, two issues that needed to be addressed were activity for hERG and muscarinic receptor M1. Introduction of a butynyl group at the N7 position of the xanthine ring gave much reduced M1 affinity with no measureable hERG activity. Linagliptin inhibits DPP-4 with an IC50=1 nM and is highly selective (>10,000-fold) against DPP-8 and DPP-9. Linagliptin shows no interactions with CYPs up to 50 mM. The described synthesis of linagliptin starts with 8-bromoxanthine, which is alkylated at the N-7 position to introduce the butyne group, followed by alkylation of the N-1 group to introduce the methyl-quinazoline group. Displacement of the bromide with (R)-Boc-3-amino-piperidine followed by deprotection gives linagliptin. When administered to db/db mice orally, linagliptin dose dependently reduced glucose excursion from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition).
Uses
Labeled Linagliptin, intended for use as an internal standard for the quantification of Linagliptin by GC- or LC-mass spectrometry.
Definition
ChEBI: A xanthine that is 7H-xanthine bearing (4-methylquinazolin-2-yl)methyl, methyl, but-2-yn-1-yl and 3-aminopiperidin-1-yl substituents at positions 1, 3, 7 and 8 respectively (the R-enantiomer). Used for treatment of type I diabetes.
Linagliptin Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| SIMSON PHARMA LIMITED | +91-8291074273 | Shanghai, India | 228 | 58 | Inquiry |
| Jigs Chemical ltd | +919099003427 | Gujarat, India | 239 | 58 | Inquiry |
| SGMR PHARMACEUTICALS PVT LTD | +91-9032001889 +91-9032001889 | Telangana, India | 83 | 58 | Inquiry |
| Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
| Bulat Pharmaceutical Pvt Ltd | +91-8448085659 +91-8448085660 | Haryana, India | 123 | 58 | Inquiry |
| SKVen Technologies Pvt.Ltd. | +91-7032295152 +91-7032295152 | Hyderabad, India | 81 | 58 | Inquiry |
| WARUKSHA LABORATORIES PVT LTD | +91-7485988764 +91-7485988764 | Gujarat, India | 77 | 58 | Inquiry |
| SUPREME DRUGS PVT LTD | +91-9924961799 +91-9924961799 | Hyderabad, India | 34 | 58 | Inquiry |
| Lewens Labs | +917043057100 | Gujarat, India | 30 | 58 | Inquiry |
| KARPSCHEM LABORATORIES | +91-7249203006 +91-7249203006 | Maharashtra, India | 786 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| SIMSON PHARMA LIMITED | 58 |
| Jigs Chemical ltd | 58 |
| SGMR PHARMACEUTICALS PVT LTD | 58 |
| Dr. Reddy's Laboratories Ltd | 58 |
| Bulat Pharmaceutical Pvt Ltd | 58 |
| SKVen Technologies Pvt.Ltd. | 58 |
| WARUKSHA LABORATORIES PVT LTD | 58 |
| SUPREME DRUGS PVT LTD | 58 |
| Lewens Labs | 58 |
| KARPSCHEM LABORATORIES | 58 |
Related articles
- What is Linagliptin?
- Linagliptin (TrajentaR, TradjentaTM, TrazentaTM, TrayentaTM) is an oral, highly selective inhibitor of dipeptidyl peptidase-4 ....
- Feb 10，2020
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