Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-akā-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione
![Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-akā-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl] purine-2,6-dione Hōʻike ʻia Kiʻi](http://cdn.globalso.com/cheerour/dadas1.png)
| inoa mea kūʻai | Linagliptin CAS NO668270-12-0 |
| Nā huaʻōlelo like | (R)-8-(3-aminopiperidin-1-yl)-7-(akā-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione; |
| CAS No | 668270-12-0 |
| ʻĀpana Molekala | C25H28N8O2 |
| Kaumaha Molekala | 472.542 |
1. ʻO Linagliptin(BI-1356) he mea hoʻopale o DPP-4, he enzyme e hoʻohaʻahaʻa i nā hormones incretin glucagon-like peptide-1 (GLP-1) a me ka 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 ʻO ,7-dihydro-1H-purine-2,6-dione kahi mea hoʻopaneʻe dipeptidyl peptidase-4 (DPP-4) no ka hoʻohana ʻana i ka mālama ʻana i ka maʻi diabetes type 2.
ʻO kā mākou hale hana ʻo Linagliptin intermediate CAS 3355-28-0, ʻenehana makua, hoʻopuka paʻa, hōʻoia maikaʻi.
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E hoʻohana: He mea hoʻopaneʻe DPP-4 koho me ka waiwai IC50 o 1 nM.
ʻO ka haʻawina in vitro: Ua kāohi ʻo Ligagliptin i ka hana DPP-4 in vitro i kekahi mau hoʻokolohua kūʻokoʻa me nā waiwai IC50 o 0.4,0.5,0.9 a me 1.1nM (mean IC50, ma kahi o 1nM).ʻO ka IC50 o ka FAP kaohi ʻana e ka liagliptin he 89 nM (ma kahi o 90-fold selectivity e pili ana iā DPP-4).
I loko o ka noiʻi vivo: I nā ʻiole kāne Wistar, nā ʻīlio Beagle a me nā monkey rhesus, ua hōʻike ʻia ʻo xanthine linagliptin i kahi mea paʻa DPP-4 maikaʻi, lōʻihi a ikaika hoʻi me> 7 h> 70% / kg ma hope o 1 mg o ka hoʻokele waha.ʻO ka hoʻokele waha o ritagliptin i nā ʻiole db / db wale nō, 45 mau minuke ma mua o ka hoʻāʻo ʻana o ka glucose waha, ua hoʻemi ʻia ka nui o ka glucose i ka plasma mai 0.1mg / kg (15% inhibition) i 1mg / kg (66% inhibition) [1] .ʻO Ligagliptin (3 a me 10mg / kg) i ka hopena i hoʻopaʻa ʻia i ka DPP-4 enzyme i ka plasma i loko o 30 mau minuke o ka hoʻokele lāʻau.ʻO Ligagliptin (1 mg / kg, po) i hōʻemi nui i ka glucose offset ma kahi o 50% [2].ʻO ka hoʻohana waha o ka DPP-4 inhibitor ligagliptin (3mg / kg, hoʻokele waha) i hōʻemi ikaika i ka hana DPP-4, hoʻopaʻa i ka GLP-1 ikaika i nā ʻeha mau, a hoʻomaikaʻi i ka hoʻōla ʻana i nā ʻiole ob / ob.I ka lā 10 ma hope o ka hōʻeha, ua hōʻike ʻia nā ʻiole ob / ob i mālama ʻia i ka liagliptin i nā ʻeha epithelialized, i hōʻike ʻia e ka nele o nā neutrophils.
Palapala: Ua ʻike ʻia a loiloi ʻia kahi papa kemika hou o ka DPP-4 inhibitors i hoʻokumu ʻia mai ka xanthine scaffold no ka mālama ʻana i ka maʻi maʻi type 2.Ua alakaʻi ʻia nā ʻano hoʻololi ʻōnaehana ʻōnaehana i ka 1 (BI 1356), kahi mea hoʻopaneʻe DPP-4 ikaika loa, koho, lōʻihi, a me ka waha e hōʻike ana i ka hoʻohaʻahaʻa nui ʻana o ka glucose koko i nā ʻano holoholona like ʻole.Ke hele nei ʻo 1 i nā hoʻāʻo ʻana o ka maʻi maʻi IIb a paʻa i ka hiki ke mālama i hoʻokahi lā i kēlā me kēia lā o ka maʻi maʻi maʻi type 2.
