Linagliptin;8-[(3R) -3-aminoperidin-1-yl] -7-ma-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione
![Linagliptin;8-[(3R) -3-aminopperidin-1-yl] -7-ma-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione egosipụtara Onyonyo](http://cdn.globalso.com/cheerour/dadas1.png)
| Aha ngwaahịa | Linagliptin CAS NO668270-12-0 |
| Ụdị okwu | (R) -8- (3-aminopperidin-1-yl) -7- (ma-2-yn-1-yl) -3-Methyl-1-((4-Methylquinazolin-2-yl) Methyl) -1H -purine-2,6 (3H,7H) -dione; |
| CAS Mba | 668270-12-0 |
| Usoro ihe omimi | C25H28N8O2 |
| Ibu molekụla | 472.542 |
1. Linagliptin (BI-1356) bụ onye na-egbochi DPP-4, enzyme nke na-eweda homonụ incretin glucagon-dị ka peptide-1 (GLP-1) na insulinotropic polypeptide (GIP) dabere na glucose.
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 bụ akwụkwọ akụkọ nwere ike na nhọrọ dipeptidyl peptidase-4 (DPP-4) inhibitor nwere ike iji na ọgwụgwọ ụdị ọrịa shuga 2.
Ụlọ ọrụ anyị rụpụtara linagliptin etiti CAS 3355-28-0, teknụzụ tozuru oke, mmepụta kwụsiri ike, mmesi obi ike.
Ọnọdụ Ndepụta Ngwaahịa: N'ahịa.
Ọ bụrụ na ị nwere mmasị na ngwaahịa anyị ma ọ bụ nwee ajụjụ ọ bụla, biko nweere onwe gị ịkpọtụrụ anyị!
A na-enye ngwaahịa ndị dị n'okpuru patent maka ebumnuche R&D naanị.
Jiri: Ọ bụ onye na-egbochi DPP-4 nke nwere ike ịhọrọ nke nwere uru IC50 nke 1 nM.
Ọmụmụ in vitro: Ligagliptin gbochiri ọrụ DPP-4 na vitro n'ọtụtụ nnwale onwe ya na ụkpụrụ IC50 nke 0.4,0.5,0.9 na 1.1nM (pụtara IC50, ihe dịka 1nM).IC50 nke mgbochi FAP site na liagliptin bụ 89 nM (ihe dịka 90-fold selectivity metụtara DPP-4).
N'ime nyocha vivo: N'ime oke Wistar nwoke, nkịta Beagle na enwe rhesus, xanthine linagliptin gosipụtara na ọ bụ ihe na-arụ ọrụ nke ọma, na-adịgide adịgide na ike DPP-4 inhibitor yana> 7 h> 70% / kg mgbe 1 mg nke nchịkwa ọnụ gasịrị.Nlekọta ọnụ nke ritagliptin na ụmụ oke db / db naanị, 45 min tupu nnwale nnabata glucose ọnụ, dabere na dose na-ebelata mgbanwe glucose plasma site na 0.1mg / kg (mmechi 15%) ruo 1mg / kg (mmechi 66%) [1] .Ligagliptin (3 na 10mg / n'arọ) dose-dabere na-egbochi enzyme DPP-4 na plasma n'ime nkeji 30 nke nchịkwa ọgwụ.Ligagliptin (1 mg / kg, po) belatara mbelata nke glucose site na ihe dịka 50% [2].Nlekọta ọnụ nke DPP-4 inhibitor ligagliptin (3mg / n'arọ, nchịkwa ọnụ) belatara ọrụ DPP-4 siri ike, mee ka GLP-1 na-arụ ọrụ na ọnya na-adịghị ala ala, yana ọgwụgwọ ka mma na ụmụ oke ob / ob.N'ụbọchị 10 mgbe mmerụ ahụ gasịrị, ụmụ oke ob / ob ndị a na-agwọ liagliptin gosipụtara ọnya epithelial nke ukwuu, nke e ji enweghị neutrophils mara.
Akwụkwọ: Achọpụtara ma nyochaa klas kemịkalụ ọhụrụ nke ndị na-egbochi DPP-4 nwere ike sitere na xanthine scaffold maka ọgwụgwọ ụdị ọrịa shuga 2.Ọdịiche nhazi usoro emela ka 1 (BI 1356), ike dị ukwuu, nhọrọ, onye na-eme ogologo oge na onye na-egbochi DPP-4 nke na-egosi mbelata glucose ọbara dị ukwuu n'ụdị anụmanụ dị iche iche.1 na-aga ule ụlọ ọgwụ nke IIb ugbu a ma na-enwe ike ọgwụgwọ otu ugboro kwa ụbọchị nke ụdị ọrịa shuga 2.
