Linagliptin;8--[(3R)-3-aminopiperidin-1-yl]-7-koma-2-ynyl-3-methyl-1--[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![Linagliptin;8--[(3R)-3-aminopiperidin-1-yl]-7-koma-2-ynyl-3-methyl-1--[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione Chithunzi](http://cdn.globalso.com/cheerour/dadas1.png)
| Dzina lazogulitsa | Linagliptin CAS NO668270-12-0 |
| Mawu ofanana ndi mawu | (R)-8-(3-aminopiperidin-1-yl)-7-(koma-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6 (3H,7H) -dione; |
| CAS No | 668270-12-0 |
| Molecular Formula | C25H28N8O2 |
| Kulemera kwa Maselo | 472.542 |
1 Linagliptin(BI-1356) ndi inhibitor ya DPP-4, puloteni yomwe imasokoneza mahomoni a incretin glucagon-like peptide-1 (GLP-1) ndi glucose-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 ndi choletsa champhamvu komanso chosankha dipeptidyl peptidase-4 (DPP-4) chomwe chingagwiritsidwe ntchito pochiza matenda amtundu wa 2.
Fakitale yathu yopanga Linagliptin wapakatikati CAS 3355-28-0, ukadaulo wokhwima, kutulutsa kokhazikika, kutsimikizika kwamtundu.
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Ntchito: Ndi yamphamvu, yosankha DPP-4 inhibitor yokhala ndi mtengo wa IC50 wa 1 nM.
Kafukufuku wa in vitro: Ligagliptin idaletsa ntchito ya DPP-4 mu vitro muzoyeserera zingapo zodziyimira pawokha ndi IC50 milingo ya 0.4,0.5,0.9 ndi 1.1nM (kutanthauza IC50, pafupifupi 1nM).IC50 ya FAP inhibition ndi liagliptin inali 89 nM (pafupifupi 90-fold selectivity poyerekeza ndi DPP-4).
Kafukufuku wa vivo: Mu makoswe aamuna a Wistar, agalu a Beagle ndi anyani a rhesus, xanthine linagliptin idawonetsedwa kuti ndi yothandiza, yolimba komanso yamphamvu ya DPP-4 inhibitor yokhala ndi> 7 h> 70% / kg pambuyo pa 1 mg yamankhwala pakamwa.Kuwongolera pakamwa kwa ritagliptin kupita ku db / db mbewa zokha, mphindi 45 musanayezetse kulolera kwa shuga m'kamwa, kudalira mlingo kumachepetsa kusintha kwa shuga m'magazi kuchokera ku 0.1mg / kg (15% choletsa) mpaka 1mg / kg (66% choletsa) [1] .Ligagliptin (3 ndi 10mg / kg) modalira mlingo adalepheretsa enzyme ya DPP-4 mu plasma mkati mwa mphindi 30 zoyendetsedwa ndi mankhwala.Ligagliptin (1 mg / kg, po) idachepetsa kwambiri kuchuluka kwa shuga ndi 50% [2].Kuwongolera pakamwa kwa DPP-4 inhibitor ligagliptin (3mg / kg, makonzedwe a pakamwa) kumachepetsa kwambiri ntchito za DPP-4, kukhazikika kwa GLP-1 yogwira ntchito m'mabala osatha, komanso kuchiritsa bwino kwa mbewa za ob / ob.Patsiku la 10 pambuyo povulala, mbewa zothandizidwa ndi liagliptin zimawonetsa mabala a epithelialized, omwe amadziwika ndi kusowa kwa neutrophils.
Chikalata: Gulu latsopano lamankhwala lamphamvu DPP-4 inhibitors lopangidwa kuchokera ku xanthine scaffold pochiza matenda a shuga a 2 lapezeka ndikuwunikidwa.Kusiyanasiyana kwadongosolo kwadzetsa 1 (BI 1356), choletsa champhamvu kwambiri, chosankha, chochita kwa nthawi yayitali, komanso chogwira pakamwa cha DPP-4 chomwe chikuwonetsa kutsika kwakukulu kwa shuga m'magazi amitundu yosiyanasiyana.1 pakali pano akuyesedwa kachipatala ka IIb ndipo ali ndi mwayi wolandira chithandizo kamodzi patsiku kwa odwala omwe ali ndi matenda amtundu wa 2.
