Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-ae-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-ae-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione Fa'aalia Ata](http://cdn.globalso.com/cheerour/dadas1.png)
| Igoa Oloa | Linagliptin CAS NO668270-12-0 |
| Synonyms | (R)-8-(3-aminopiperidin-1-yl)-7-(ae-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione; |
| CAS Nu | 668270-12-0 |
| Fuafua mole | C25H28N8O2 |
| Molecular Weight | 472.542 |
1. Linagliptin(BI-1356) o se inhibitor o le DPP-4, o se enzyme e faʻaleagaina ai le incretin hormones glucagon-like peptide-1 (GLP-1) ma le glucose-dependent insulinotropic polypeptide (GIP).
2. 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butyn-1-yl)-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-3 ,7-dihydro-1H-purine-2,6-dione o se mea fou malosi ma filifili le dipeptidyl peptidase-4 (DPP-4) inhibitor ma mafai ona faʻaaogaina i togafitiga o le maʻisuka ituaiga 2.
O la matou falegaosimea o loʻo gaosia le Linagliptin intermediate CAS 3355-28-0, tekinolosi matua, gaosiga mautu, faʻamautinoaga lelei.
Tulaga Fa'amaumauga : O lo'o iai Fa'atauga.
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O oloa i lalo o pateni e ofoina atu mo na'o le R & D.
Fa'aoga: O se fa'atosina malosi, filifili DPP-4 fa'atasi ma le tau IC50 o le 1 nM.
Suʻesuʻega in vitro: Ligagliptin faʻasaina le DPP-4 gaioiga in vitro i le tele o faʻataʻitaʻiga tutoʻatasi ma IC50 tau o le 0.4,0.5,0.9 ma le 1.1nM (o lona uiga IC50, tusa ma le 1nM).O le IC50 o le faʻasaina o le FAP e le liagliptin e 89 nM (pe a ma le 90-filifili le filifilia e faʻatatau i le DPP-4).
I suʻesuʻega i vivo: I tamaʻi Wistar rats, Beagle dogs ma rhesus manuki, xanthine linagliptin na faʻaalia e avea o se inhibitor DPP-4 lelei, umi ma malosi ma> 7 h> 70% / kilokalama pe a maeʻa le 1 mg o le tuʻu gutu.O le tuʻuina atu o le ritagliptin i le db / db isumu naʻo ia, 45 minute aʻo leʻi faia le suʻega o le faʻapalepale o le kulukose, faʻalagolago i le faʻaogaina o le faʻaitiitia o le suiga o le kulukose plasma mai le 0.1mg / kg (15% inhibition) i le 1mg / kg (66% inhibition) [1] .O le Ligagliptin (3 ma le 10mg / kg) faʻatatau-faʻalagolago e taofia ai le DPP-4 enzyme i le plasma i totonu o le 30 minute o le faʻaaogaina o fualaau faasaina.Ligagliptin (1 mg / kilokalama, po) faʻaititia tele le kulukose faʻafefe e tusa ma le 50% [2].O le faʻaogaina o le DPP-4 inhibitor ligagliptin (3mg / kilokalama, faʻatonuga tautala) faʻaitiitia malosi le gaioiga DPP-4, faʻamautu le GLP-1 malosi i manuʻa tumau, ma faʻaleleia le faʻamalolo i isumu.I le aso 10 ina ua maeʻa manuʻa, o isumu na togafitia i le liagliptin na faʻaalia ai le tele o manuʻa epithelialized, faʻaalia i le leai o ni neutrophils.
Pepa: Ua maua ma iloiloina se vaega fou o vaila'au fa'amalosi DPP-4 fa'atosina e maua mai le fa'amanu xanthine mo togafitiga o le ma'isuka ituaiga 2.O suiga fa'atulagaina fa'atulagaina ua o'o atu ai i le 1 (BI 1356), o se fa'ato'aga DPP-4 e sili ona malosi, filifili, umi, ma tautala fa'amalosi e fa'aalia ai le fa'aitiitia tele o le kulukose toto i ituaiga meaola eseese.1 o loʻo faʻataʻitaʻiina nei faʻataʻitaʻiga IIb faʻataʻitaʻiga ma o loʻo iai le avanoa mo togafitiga faʻatasi i aso uma o le maʻisuka ituaiga 2.
