Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione
![Linagliptin;8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]purine-2,6-dione E Hlahiswa Setšoantšo](http://cdn.globalso.com/cheerour/dadas1.png)
| Lebitso la Sehlahiswa | Linagliptin CAS NO668270-12-0 |
| Litlhaloso tse tšoanang | (R)-8-(3-aminopiperidin-1-yl)-7-(empa-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6 (3H,7H) -dione; |
| Nomoro ea CAS | 668270-12-0 |
| Foromo ea limolek'hule | C25H28N8O2 |
| Boima ba Molek'hule | 472.542 |
1. Linagliptin(BI-1356) ke inhibitor ea DPP-4, enzyme e theolang lihomone tsa incretin glucagon-like peptide-1 (GLP-1) le glucose-based 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 ke inhibitor e ncha e matla le e khethang ea dipeptidyl peptidase-4 (DPP-4) e ka sebelisoang kalafong ea lefu la tsoekere la mofuta oa 2.
CAS 3355-28-0 ea moetsi oa feme ea rona, CAS 3355-28-0, theknoloji e holileng, tlhahiso e tsitsitseng, netefatso ea boleng.
Boemo ba Inventory : Ho Stock.
Haeba u thahasella lihlahisoa tsa rona kapa u na le lipotso, ka kopo ikutloe u lokolohile ho ikopanya le rona!
Lihlahisoa tse tlas'a patent li fanoa molemong oa R&D feela.
Sebelisa: Ke inhibitor e matla, e khethang ea DPP-4 e nang le boleng ba IC50 ba 1 nM.
Thuto ea in vitro: Ligagliptin e thibetse ts'ebetso ea DPP-4 in vitro litekong tse 'maloa tse ikemetseng tse nang le boleng ba IC50 ba 0.4,0.5,0.9 le 1.1nM (e bolela IC50, e ka bang 1nM).IC50 ea inhibition ea FAP ka liagliptin e ne e le 89 nM (khetho e ka bang makhetlo a 90 e amanang le DPP-4).
Lipatlisiso tsa in vivo: Likhotong tse tona tsa Wistar, lintja tsa Beagle le litšoene tsa rhesus, xanthine linagliptin e bontšitsoe e le inhibitor e sebetsang hantle, e tšoarellang le e matla ea DPP-4 e nang le> 7 h> 70% / kg ka mor'a 1 mg ea tsamaiso ea molomo.Ts'ebeliso ea molomo ea ritagliptin ho litoeba tsa db / db feela, metsotso e 45 pele ho tlhahlobo ea mamello ea tsoekere ea molomo, ho itšetlehile ka tekanyo e fokotsitseng ho tloha ho 0.1mg / kg (15% inhibition) ho ea ho 1mg / kg (66% inhibition) [1] .Ligagliptin (3 le 10mg / kg) e itšetlehile ka tekanyo ea enzyme ea DPP-4 ho plasma nakong ea metsotso e 30 ea tsamaiso ea lithethefatsi.Ligagliptin (1 mg / kg, po) e fokolitse ho fokotseha ha tsoekere haholo ka hoo e ka bang 50% [2].Tsamaiso ea molomo ea DPP-4 inhibitor ligagliptin (3mg / kg, tsamaiso ea molomo) e fokolitse ts'ebetso ea DPP-4 ka matla, e tsitsitse GLP-1 e sebetsang ka maqeba a sa foleng, le pholiso e ntlafetseng ho litoeba tsa ob / ob.Ka letsatsi la 10 ka mor'a kotsi, litoeba tse tšoaroang ke liagliptin li ile tsa bontša maqeba a epithelialized, a khetholloang ke ho ba sieo ha li-neutrophils.
Tokomane: Sehlopha se secha sa lik'hemik'hale sa li-inhibitors tsa DPP-4 tse matla tse nkiloeng ho xanthine scaffold bakeng sa kalafo ea lefu la tsoekere la mofuta oa 2 li se li fumanoe le ho hlahlojoa.Liphetoho tse fapaneng tsa sebopeho li lebisitse ho 1 (BI 1356), inhibitor e matla haholo, e khethang, e tšoarellang nako e telele, le e sebetsang ka molomo ea DPP-4 e bonts'ang phokotseho e kholo ea tsoekere maling mefuteng e fapaneng ea liphoofolo.1 hajoale e ntse e le litekong tsa kliniki tsa IIb mme e na le monyetla oa kalafo ea hang ka letsatsi ea lefu la tsoekere la mofuta oa 2.
