Linagliptin;8-[(3R) -3-aminopiperidin-1-yl] -7-sed-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)myl]purinum-2,6-dione
Product Name | Linagliptin CAS NO668270-12-0 |
Synonyma | (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; |
CAS No | 668270-12-0 |
Formulae hypotheticae | C25H28N8O2 |
M. Pondus | 472.542 |
1. Linagliptin (BI-1356) est inhibitor of DPP-4, enzyme quod hormones glucagonos peptidis-I (GLP-1) insulinotropico (GIP) dependens et incretino glucagono recedit.
2. 8-[(3R) -3-Amino-1-piperidinyl]-7-(2-butyn-1-yl) -3-methyl-1-[(4-methyl-2-quinazolinyl) methyl]-3 ,7-dihydro-1H-purini-2,6-dione nova potens et selectiva dipeptidyla peptidase-4 (DPP-4) inhibitor usui potentiali in tractatione generis 2 diabete est.
Nostra fabrica fabricandi Linagliptin intermedium CAS 3355-28-0, technicae maturae, output stabile, qualitas certitudinis.
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Usus: Potens, selectiva DPP-4 inhibitor cum valore IC50 1 nM.
In vitro studio: Ligagliptin in vitro inhibuit DPP-4 actio in pluribus experimentis independentibus cum IC50 valoribus 0.4,0.5,0.9 et 1.1nM (medium IC50, circiter 1nM).IC50 of FAP inhibitionis per liagliptin 89 nM (circa 90-duplicem selectivity DPP-IV relatis).
In investigationibus vivo: Mures in Wistar, Beagle canes et simiae rhesi, xanthine linagliptin ostensae sunt efficientem, durabilem et potentem DPP-4 inhibitorem cum >7 h> 70% / kg post 1 mg administrationis oralis.Administratio oralis ritagliptin ad db / db mures tantum, 45 min ante tolerantiam glucosi oris experimentum, dosis dependenter reducta plasma glucosi transpositio ab 0.1mg / kg (15% inhibitionis) ad 1mg / kg (66% inhibitionis) [1]. .Ligagliptin (3 et 10mg / kg) doses dependenter inhibuit DPP-4 enzyme in plasmate intra 30 min medicamentorum administrationis.Ligagliptin (1 mg / kg, po) cingulum glucosum significanter reductum per circiter 50% [2].Administratio oralis inhibitoris ligagliptin inhibitoris (3mg / kg, administratio oralis) valde diminuta est DPP-4 actio, stabilita GLP-1 activa in vulneribus chronicis, et sanatio in ob / ob muribus aucta.Ad diem X post-iniuriam, ob mures liagliptin affectos plerunque vulnera epithelialata, absentia neutrophils notata, ostendit.
Documentum: Novum genus chemicorum potentium DPP-4 inhibitorum structuraliter e catasta xanthine derivatum ad tractationem diabetarum specierum 2 diabetarum inventa et aestimata est.Variationes structurales systematicae ad 1 (BI 1356) perduxerunt, potentissimum, selectivum, longum activum, et viva voce inhibitorem DPP-4, qui sanguinem glucosum in diversis speciebus animali demissis satis ostendit.1 nunc orci periodum IIb iudiciis sustinens et potentialem ad tractationem 2 diabeticorum semel cottidianam tractationem tenet.