Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-engari-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-engari-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione e whakaatuhia ana Whakaahua](http://cdn.globalso.com/cheerour/dadas1.png)
| Ingoa Hua | Linagliptin CAS NO668270-12-0 |
| Nga kupu taurite | (R)-8-(3-aminopiperidin-1-yl)-7-(engari-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione; |
| CAS No | 668270-12-0 |
| Tātai rāpoi | C25H28N8O2 |
| Taumaha rāpoi | 472.542 |
1. Ko te Linagliptin(BI-1356) he aukati i te DPP-4, he whākōkī e whakaheke ana i nga homoni incretin glucagon-like peptide-1 (GLP-1) me te 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 Ko te 7-dihydro-1H-purine-2,6-dione he pukapuka kaha me te whiriwhiri i te aukati dipeptidyl peptidase-4 (DPP-4) me te whakamahi pea ki te maimoatanga o te mate huka momo 2.
Ko ta matou wheketere hanga Linagliptin takawaenga CAS 3355-28-0, te hangarau pakeke, te putanga pumau, te whakapumautanga o te kounga.
Tūnga Inventory : Kei te Raarangi.
Mena kei te pirangi koe ki a maatau hua, he patai ranei, tena koa whakapiri mai ki a maatau!
Ko nga hua kei raro i te patent ka tukuna mo te kaupapa R&D anake.
Whakamahia: He kaha, he aukati DPP-4 whiriwhiri me te uara IC50 o te 1 nM.
Te rangahau in vitro: I aukati a Ligagliptin i nga mahi DPP-4 in vitro i roto i nga whakamatautau motuhake me nga uara IC50 o 0.4,0.5,0.9 me 1.1nM (te tikanga IC50, tata ki te 1nM).Ko te IC50 o te aukati FAP na te liagliptin he 89 nM (mo te 90-fold te whiriwhiringa e pa ana ki te DPP-4).
I roto i te rangahau vivo: I roto i nga kiore Wistar tane, nga kuri Beagle me nga makimaki rhesus, ko te xanthine linagliptin i whakaatuhia he pai, he roa, he kaha te aukati DPP-4 me te> 7 h> 70% / kg i muri i te 1 mg o te whakahaere waha.Ko te whakahaere a-waha o te ritagliptin ki nga kiore db / db anake, 45 min i mua i te whakamatautau o te manawanui o te huka toto, na runga i te horopeta-whakaheke i te nekehanga huka plasma mai i te 0.1mg / kg (15% te aukati) ki te 1mg / kg (66% te aukati) [1] .Ko te Ligagliptin (3 me te 10mg / kg) i runga i te horopeta-i te aukati i te DPP-4 enzyme i roto i te plasma i roto i te 30 meneti i muri i te whakahaerenga tarukino.Ko te Ligagliptin (1 mg / kg, po) i tino whakahekehia te hukahuka ma te 50% [2].Ko te whakahaere a-waha o te DPP-4 inhibitor ligagliptin (3mg / kg, te whakahaere waha) i tino whakahekehia te mahi DPP-4, te whakapumau i te GLP-1 kaha i roto i nga patunga mau tonu, me te pai ake o te whakaora i nga kiore ob / ob.I te ra 10 i muri i te wharanga, ko nga kiore ob / ob kua rongoahia e te liagliptin te nuinga o nga patunga epithelialized, he tohu na te kore o nga neutrophils.
Tuhinga: Kua kitea he karaehe matū hou o nga aukati DPP-4 kaha i ahu mai i te scaffold xanthine mo te maimoatanga o te mate huka momo 2 kua kitea me te arotake.Ko nga rereketanga o te hanganga nahanaha kua arai ki te 1 (BI 1356), he aukati DPP-4 tino kaha, whiriwhiri, roa, me te kaha o te waha e whakaatu ana i te whakaheke toto huka toto i roto i nga momo kararehe rereke.Kei te haere a 1 ki nga whakamatautau haumanu IIb i tenei wa me te pupuri i te kaha mo te maimoatanga kotahi ia ra mo nga turoro mate huka momo 2.
