I-Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-kodwa-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![I-Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-kodwa-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione Okufakiwe Isithombe](http://cdn.globalso.com/cheerour/dadas1.png)
| Igama Lomkhiqizo | I-Linagliptin CAS NO668270-12-0 |
| Omqondofana | (R)-8-(3-aminopiperidin-1-yl)-7-(kodwa-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H) -dione; |
| Inombolo ye-CAS | 668270-12-0 |
| I-Molecular Formula | I-C25H28N8O2 |
| Isisindo samangqamuzana | 472.542 |
1. I-Linagliptin(BI-1356) iyisivimbeli se-DPP-4, i-enzyme eyehlisa amahomoni e-incretin i-glucagon-like peptide-1 (GLP-1) kanye ne-insulinotropic polypeptide (GIP) encike ku-glucose.
2. 8-[(3R)-3-Amino-1-piperidinyl]-7-(2-butyn-1-yl)-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-3 I-7-dihydro-1H-purine-2,6-dione iyi-novel enamandla futhi ekhethiwe ye-dipeptidyl peptidase-4 (DPP-4) inhibitor engase isetshenziswe ekwelapheni isifo sikashukela sohlobo 2.
Umkhiqizi wethu wefekthri i-Linagliptin emaphakathi i-CAS 3355-28-0, ubuchwepheshe obuvuthiwe, ukuphuma okuzinzile, ukuqinisekiswa kwekhwalithi.
Isimo Sokusungula : Esitokweni.
Uma unentshisekelo ngemikhiqizo yethu noma unemibuzo, sicela ukhululeke ukuxhumana nathi!
Imikhiqizo engaphansi kwelungelo lobunikazi inikezwa inhloso ye-R & D kuphela.
Sebenzisa: Kuyi-DPP-4 inhibitor enamandla, ekhethiwe enenani le-IC50 elingu-1 nM.
Ucwaningo lwe-in vitro: I-Ligagliptin ivimbe umsebenzi we-DPP-4 ku-vitro ezivivinyweni ezimbalwa ezizimele ezinamavelu e-IC50 angu-0.4,0.5,0.9 kanye ne-1.1nM (isho i-IC50, cishe i-1nM).I-IC50 ye-FAP inhibition nge-liagliptin yayingu-89 nM (cishe ukukhetha okungu-90 ngokuhlobene ne-DPP-4).
Ocwaningweni lwe-vivo: Emagundaneni angama-Wistar wesilisa, ezinjeni ze-Beagle nezinkawu ze-rhesus, i-xanthine inagliptin yaboniswa iyisivimbi esisebenzayo, esiqinile futhi esinamandla se-DPP-4 esine-> 7 h> 70% / kg ngemva kwe-1 mg yokuphathwa ngomlomo.Ukuphathwa ngomlomo kwe-ritagliptin kuya ku-db / db amagundane kuphela, imizuzu engama-45 ngaphambi kokuhlolwa kokubekezelela i-glucose ngomlomo, ngokuncika komthamo kunciphise ukushintshwa kwe-glucose ku-plasma kusuka ku-0.1mg / kg (15% inhibition) kuya ku-1mg / kg (66% inhibition) [1] .I-Ligagliptin (i-3 kanye ne-10mg / kg) incike kumthamo ivimbele i-enzyme ye-DPP-4 ku-plasma kungakapheli imizuzu engama-30 yokuphathwa kwezidakamizwa.I-Ligagliptin (1 mg/kg, po) yehlise kakhulu ukuncishiswa kwe-glucose cishe ngama-50% [2].Ukuphathwa ngomlomo kwe-DPP-4 inhibitor ligagliptin (3mg / kg, ukuphathwa ngomlomo) kunciphise kakhulu umsebenzi we-DPP-4, kuzinziswe i-GLP-1 esebenzayo emanxebeni angapheli, kanye nokuphulukiswa okuthuthukisiwe kumagundane we-ob / ob.Ngosuku lwe-10 ngemuva kokulimala, amagundane alashwe nge-liagliptin ob/ob abonise amanxeba amaningi e-epithelialized, abonakala ngokungabikho kwama-neutrophils.
Idokhumenti: Ikilasi elisha lamakhemikhali lama-DPP-4 inhibitors anamandla asuselwa ku-xanthine scaffold yokwelapha isifo sikashukela sohlobo 2 selitholakele futhi lahlolwa.Ukwehluka kwesakhiwo okuhlelekile kuholele ku-1 (BI 1356), i-DPP-4 inhibitor enamandla kakhulu, ekhethayo, esebenza isikhathi eside, futhi esebenza ngomlomo ebonisa ukwehla okukhulu kweglucose ezinhlobonhlobo zezilwane.I-1 okwamanje yenza uhlolo lwesigaba se-IIb somtholampilo futhi inamandla okwelashwa kanye ngosuku kohlobo 2 lwesifo sikashukela.
