Linagliptin
- $5 - $5450
- Product name: Linagliptin
- CAS: 668270-12-0
- MF: C25H28N8O2
- MW: 472.54
- EINECS:1308068-626-2
- MDL Number:MFCD14635356
- Synonyms:linagliptin;(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;1H-Purine-2,6-dione, 8-((3R)-3-amino-1-piperidinyl)-7-(2-butynyl)-3,7-dihydro-3-methyl-1-((4-methyl-2-quinazolinyl)methyl)-;Bi 1356;Ondero;8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-dione;8-[(3R)-3-AMino-1-piperidinyl]-7-(2-butynyl)-3,7-dihydro-3-Methyl-1-[(4-Methyl-2-quinazolinyl)Methyl]-1H-purine-2,6-d;8-[(3R)-3-aMinopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-Methyl-1-[(4-Methylquinazolin-2-yl)Methyl]-2,3,6,7-tetrahydro-1H-purine-2,6-dione
36 prices
Selected condition:
Brand
- Activate Scientific
- Adipogen Life Sciences
- AK Scientific
- Ambeed
- American Custom Chemicals Corporation
- ApexBio Technology
- Axon Medchem
- Biorbyt Ltd
- Biosynth Carbosynth
- Cayman Chemical
- ChemScene
- Chemtos
- DC Chemicals
- Matrix Scientific
- Medical Isotopes, Inc.
- TRC
Package
- 5mg
- 10mg
- 25mg
- 50mg
- 100mg
- 250mg
- 500mg
- 1g
- 5G
- 10g
- 25g
- ManufacturerActivate Scientific
- Product numberAS18223
- Product descriptionLinagliptin 96%
- Packaging250mg
- Price$34
- Updated2021-12-16
- Buy
- ManufacturerActivate Scientific
- Product numberAS18223
- Product descriptionLinagliptin 96%
- Packaging1g
- Price$86
- Updated2021-12-16
- Buy
- ManufacturerActivate Scientific
- Product numberAS18223
- Product descriptionLinagliptin 96%
- Packaging5G
- Price$191
- Updated2021-12-16
- Buy
- ManufacturerActivate Scientific
- Product numberAS18223
- Product descriptionLinagliptin 96%
- Packaging25g
- Price$641
- Updated2021-12-16
- Buy
- ManufacturerAdipogen Life Sciences
- Product numberAG-CR1-3618-M050
- Product descriptionLinagliptin ≥98%(HPLC)
- Packaging50mg
- Price$90
- Updated2021-12-16
- Buy
- ManufacturerAK Scientific
- Product numberX1062
- Product descriptionLinagliptin
- Packaging1g
- Price$109
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging25g
- Price$476
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging10g
- Price$286
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging5g
- Price$145
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging1g
- Price$49
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging250mg
- Price$34
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging100mg
- Price$18
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging50mg
- Price$11
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging10mg
- Price$7
- Updated2021-12-16
- Buy
- ManufacturerAmbeed
- Product numberA392251
- Product description(R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+%
- Packaging5mg
- Price$5
- Updated2021-12-16
- Buy
- ManufacturerAmerican Custom Chemicals Corporation
- Product numberAPI0007204
- Product descriptionLINAGLIPTIN 95.00%
- Packaging5MG
- Price$510
- Updated2021-12-16
- Buy
Manufacturer | Product number | Product description | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|
Activate Scientific | AS18223 | Linagliptin 96% | 250mg | $34 | 2021-12-16 | Buy |
Activate Scientific | AS18223 | Linagliptin 96% | 1g | $86 | 2021-12-16 | Buy |
Activate Scientific | AS18223 | Linagliptin 96% | 5G | $191 | 2021-12-16 | Buy |
Activate Scientific | AS18223 | Linagliptin 96% | 25g | $641 | 2021-12-16 | Buy |
Adipogen Life Sciences | AG-CR1-3618-M050 | Linagliptin ≥98%(HPLC) | 50mg | $90 | 2021-12-16 | Buy |
AK Scientific | X1062 | Linagliptin | 1g | $109 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 25g | $476 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 10g | $286 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 5g | $145 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 1g | $49 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 250mg | $34 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 100mg | $18 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 50mg | $11 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 10mg | $7 | 2021-12-16 | Buy |
Ambeed | A392251 | (R)-8-(3-Aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione 98+% | 5mg | $5 | 2021-12-16 | Buy |
American Custom Chemicals Corporation | API0007204 | LINAGLIPTIN 95.00% | 5MG | $510 | 2021-12-16 | Buy |
Properties
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
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 Information
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Signal word: | Warning | ||||||||||||||||||||||||||||
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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).More related product prices
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Suppliers and manufacturers
Protheragen-ING