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 Inoratidzirwa Image](http://cdn.globalso.com/cheerour/dadas1.png)
| Product Name | Linagliptin CAS NO668270-12-0 |
| Mashoko anoreva zvakafanana | (R)-8-(3-aminopiperidin-1-yl)-7-(asi-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione; |
| CAS Nha | 668270-12-0 |
| Molecular Formula | C25H28N8O2 |
| Molecular Weight | 472.542 |
1. Linagliptin(BI-1356) inhibitor yeDPP-4, enzyme inoderedza incretin hormones glucagon-like peptide-1 (GLP-1) uye glucose-inotsamira 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 inhibitor ine simba uye inosarudza dipeptidyl peptidase-4 (DPP-4) inogona kushandiswa mukurapa chirwere cheshuga chechipiri.
Yedu fekitori inogadzira Linagliptin yepakati CAS 3355-28-0, yakakura tekinoroji, yakagadzika kubuda, simbisiro yemhando.
Inventory Status : In Stock.
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Shandisa: Iine simba, inosarudza DPP-4 inhibitor ine IC50 kukosha kwe1 nM.
In vitro kudzidza: Ligagliptin inhibited DPP-4 chiitiko mu vitro mune akati wandei akazvimirira kuyedza neIC50 kukosha kwe0.4,0.5,0.9 uye 1.1nM (kureva IC50, ingangoita 1nM).Iyo IC50 yeFAP inhibition neliagliptin yaive 89 nM (inenge makumi mapfumbamwe-fold selectivity inoenderana neDPP-4).
In vivo tsvagiridzo: Muhurume Wistar makonzo, imbwa dzeBeagle uye rhesus tsoko, xanthine linagliptin yakaratidzwa kuva inoshanda, inogara uye ine simba DPP-4 inhibitor ine> 7 h> 70% / kg mushure me1 mg yekutonga nemuromo.Kudzorwa nemuromo kwe ritagliptin kune db / db mbeva chete, 45 maminetsi isati yaitwa yemuromo glucose kushivirira bvunzo, dose-zvichienderana nekuderedza plasma glucose kuchinja kubva 0.1mg / kg (15% inhibition) kusvika 1mg / kg (66% inhibition) [1] .Ligagliptin (3 uye 10mg / kg) dosi-yakavharira iyo DPP-4 enzyme muplasma mukati me30 maminetsi ekutonga zvinodhaka.Ligagliptin (1 mg / kg, po) yakaderedza zvakanyanya glucose kuderedzwa ne50% [2].Oral administration yeDPP-4 inhibitor ligagliptin (3mg / kg, oral administration) yakaderedza zvakasimba DPP-4 chiitiko, yakagadzikana inoshanda GLP-1 mumaronda asingagumi, uye kuporesa kuporesa mu ob / ob mbeva.Pazuva 10 mushure mekukuvara, liagliptin-yakarapwa ob / ob mbeva yairatidza kazhinji epithelialized maronda, anoratidzwa nekushaikwa kwemaneutrophils.
Gwaro: Mushonga mutsva wemakemikari kirasi yeane simba DPP-4 inhibitors akaumbwa kubva kuxanthine scaffold yekurapwa kwemhando ye2 chirwere cheshuga yakawanikwa uye yakaongororwa.Kurongeka kwakasiyana-siyana kwakakonzera ku1 (BI 1356), yakasimba kwazvo, inosarudza, inogara kwenguva refu, uye nemuromo inoshanda DPP-4 inhibitor inoratidza kuderera kweglucose yeropa mumhando dzakasiyana dzemhuka.1 parizvino irikuitwa kiriniki yechikamu IIb miedzo uye inobata mukana wekurapwa kamwe chete pazuva kwerudzi rwechipiri rwechirwere cheshuga.
