Linagliptin;8 - [(3R) -3-aminopiperidin-1-yl] -7-ariko-2-ynyl-3-methyl-1 - [((4
![Linagliptin;8 - [(3R) -3-aminopiperidin-1-yl] -7-ariko-2-ynyl-3-methyl-1 - Ishusho](http://cdn.globalso.com/cheerour/dadas1.png)
| izina RY'IGICURUZWA | Linagliptin CAS NO668270-12-0 |
| Synonyme | (R) -8- ((3 -purine-2,6 (3H, 7H) -dione; |
| CAS No. | 668270-12-0 |
| Inzira ya molekulari | C25H28N8O2 |
| Uburemere bwa molekile | 472.542 |
1. Linagliptin (BI-1356) ni inhibitori ya DPP-4, enzyme itesha agaciro imisemburo ya incretin glucagon imeze nka peptide-1 (GLP-1) na glucose iterwa na insulineotropique polypeptide (GIP).
2. 8 - [(3R) -3-Amino-1-piperidinyl] -7- (2-butyn-1-yl) -3-methyl-1 - , 7-dihydro-1H-purine-2,6-dione nigitabo gishya kandi gitoranya dipeptidyl peptidase-4 (DPP-4) inhibitor ifite ubushobozi bwo kuvura diyabete yo mu bwoko bwa 2.
Uruganda rwacu rwa Linagliptin rwagati CAS 3355-28-0, tekinoroji ikuze, umusaruro uhamye, ubwishingizi bufite ireme.
Ibarurishamibare: Mububiko.
Niba ushimishijwe nibicuruzwa byacu cyangwa ufite ikibazo, nyamuneka twandikire!
Ibicuruzwa biri muri patenti bitangwa kubwintego ya R & D gusa.
Koresha: Nibikoresho bikomeye, byatoranijwe DPP-4 inhibitor ifite IC50 agaciro ka 1 nM.
Mu bushakashatsi bwa vitro: Ligagliptin yabujije ibikorwa bya DPP-4 muri vitro mu bushakashatsi bwinshi bwigenga bufite agaciro ka IC50 ka 0.4,0.5,0.9 na 1.1nM (bivuze IC50, hafi 1nM).IC50 yo kubuza FAP na liagliptin yari 89 nM (guhitamo inshuro 90 ugereranije na DPP-4).
Mu bushakashatsi bwa vivo: Mu mbeba za Wistar z’abagabo, imbwa za Beagle n’inguge za rhesus, xanthine linagliptin yerekanwe ko ikora neza, iramba kandi ikomeye DPP-4 inhibitor hamwe na> 7 h> 70% / kg nyuma ya mg 1 yubuyobozi bwo mu kanwa.Ubuyobozi bwo mu kanwa bwa ritagliptine kugeza imbeba ya db / db yonyine, 45 min mbere yikizamini cyo kwihanganira glucose yo mu kanwa, biterwa na dose glucose yagabanutse kuva 0.1mg / kg (15% kubuza) kugera kuri 1mg / kg (kubuza 66%) [1] .Ligagliptin (3 na 10mg / kg) ikoresheje urugero rwabujije enzyme ya DPP-4 muri plasma mu minota 30 yo kunywa ibiyobyabwenge.Ligagliptin (1 mg / kg, po) yagabanije cyane glucose kugabanuka hafi 50% [2].Ubuyobozi bwo mu kanwa bwa DPP-4 inhibitor ligagliptin (3mg / kg, ubuyobozi bwo mu kanwa) bwagabanije cyane ibikorwa bya DPP-4, bihindura GLP-1 ikora mu bikomere bidakira, no kunoza gukira kwimbeba za ob / ob.Ku munsi wa 10 nyuma yimvune, imbeba za liagliptin zavuwe na ob / ob zerekanaga ahanini ibikomere bya epiteliyale, byaranzwe no kutagira neutrophile.
Inyandiko: Icyiciro gishya cyimiti cyimbaraga za DPP-4 inhibitor zubatswe muburyo bukomoka kuri xanthine scafold yo kuvura diyabete yo mu bwoko bwa 2 yavumbuwe kandi irasuzumwa.Imiterere ihindagurika itunganijwe yatumye abantu 1 (BI 1356), imbaraga zikomeye, zitoranya, zikora igihe kirekire, kandi zikora mu kanwa DPP-4 yerekana uburyo glucose yamaraso igabanuka mubwoko butandukanye bwinyamaswa.1 kuri ubu arimo gukorerwa ibizamini byo mu cyiciro cya IIb kandi afite ubushobozi bwo kuvura rimwe na rimwe buri munsi abarwayi ba diyabete yo mu bwoko bwa 2.
