iLinagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-kodwa-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![iLinagliptin;8--[(3R)-3-aminopiperidin-1-yl]-7-kodwa-2-ynyl-3-methyl-1--[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione efakiweyo Umfanekiso](http://cdn.globalso.com/cheerour/dadas1.png)
| Igama lemveliso | Linagliptin CAS NO668270-12-0 |
| Izithethantonye | (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 yeCAS | 668270-12-0 |
| Ifomula yeemolekyuli | C25H28N8O2 |
| Ubunzima beMolekyuli | 472.542 |
1. I-Linagliptin(BI-1356) yi-inhibitor ye-DPP-4, i-enzyme ethoba i-incretin hormones i-glucagon-like peptide-1 (GLP-1) kunye ne-glucose-exhomekeke kwi-insulinotropic polypeptide (GIP).
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 iyinoveli enamandla kunye ne-dipeptidyl peptidase-4 (DPP-4) inhibitor ekhethiweyo kunye nokusetyenziswa okunamandla kunyango lwe-2 yeswekile.
Umzi-mveliso wethu weLinagliptin ophakathi we-CAS 3355-28-0, itekhnoloji evuthiweyo, iziphumo ezizinzileyo, uqinisekiso lomgangatho.
Ubume be-Inventory : KwiStokhwe.
Ukuba unomdla kwiimveliso zethu okanye unemibuzo, nceda uzive ukhululekile ukuqhagamshelana nathi!
Iimveliso eziphantsi kwelungelo elilodwa lomenzi wechiza zibonelelwa ngeenjongo zeR & D kuphela.
Sebenzisa: Inamandla, i-DPP-4 inhibitor ekhethiweyo kunye nexabiso le-IC50 le-1 nM.
Uphononongo lwe-in vitro: I-Ligagliptin inhibite umsebenzi we-DPP-4 kwi-vitro kwiimvavanyo ezininzi ezizimeleyo ezinexabiso le-IC50 le-0.4,0.5,0.9 kunye ne-1.1nM (ithetha i-IC50, malunga ne-1nM).I-IC50 ye-FAP inhibition yi-liagliptin yayingu-89 nM (malunga ne-90-fold selectivity ngokumalunga ne-DPP-4).
Uphando lwe-vivo: Kwiigundane ze-Wistar zamadoda, izinja ze-Beagle kunye neenkawu ze-rhesus, i-xanthine linagliptin ibonakaliswe njenge-inhibitor ye-DPP-4 esebenzayo, ehlala ixesha elide kunye ne> 7 h> 70% / kg emva kwe-1 mg yokulawulwa komlomo.Ulawulo lomlomo lwe-ritagliptin ukuya kwi-db / db iimpuku zodwa, kwimizuzu engama-45 phambi kovavanyo lokunyamezela iswekile yomlomo, ngokuxhomekeka kwidosi kuncitshiswe utshintsho lweglucose kwiplasma ukusuka ku-0.1mg/kg (15% inhibition) ukuya kwi-1mg/kg (66% inhibition) [1] .I-Ligagliptin (i-3 kunye ne-10mg / kg) i-dose-ixhomekeke ngokuxhomekeke kwi-enzyme ye-DPP-4 kwi-plasma ngaphakathi kwe-30 min yokulawula ichiza.I-Ligagliptin (1 mg / kg, po) iyancipha kakhulu i-glucose offset malunga ne-50% [2].Ukulawulwa komlomo kwe-DPP-4 inhibitor ligagliptin (3mg / kg, ulawulo lomlomo) yanciphisa kakhulu umsebenzi we-DPP-4, izinzile i-GLP-1 esebenzayo kumanxeba angapheliyo, kunye nokuphucula ukuphilisa kwi-ob / ob mice.Ngomhla we-10 emva kokwenzakala, iimpuku ze-liagliptin ezinyangelwe i-ob / ob zabonisa ubukhulu becala amanxeba e-epithelialized, abonakaliswa kukungabikho kwe-neutrophils.
Uxwebhu: Iklasi entsha yeekhemikhali ze-DPP-4 inhibitors ezinamandla ezithathwe kwi-scaffold ye-xanthine yonyango lwe-2 yeswekile iye yafunyanwa kwaye yavavanywa.Iinguqu ezicwangcisiweyo ezicwangcisiweyo ziye zakhokelela kwi-1 (BI 1356), i-inhibitor enamandla kakhulu, ekhethiweyo, esebenza ixesha elide, kunye ne-DPP-4 yomlomo ebonisa ukuhla kwe-glucose eninzi kwiintlobo zezilwanyana ezahlukeneyo.I-1 okwangoku iphantsi kovavanyo lwesigaba se-IIb seklinikhi kwaye ibambe amandla okunyangwa kanye ngosuku lwe-2 yesifo seswekile.
