Linagliptin;8-[(3R) -3-aminoperidin-1-yl] -7-amma-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione

Linagliptin;8-[(3R) -3-aminopperidin-1-yl] -7-amma-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione Featured Hoto

taƙaitaccen bayanin:

Chemical & Jiki Properties

Category: Pharmaceutical albarkatun kasa;Mai hanawa;Amines;Aromatics;Heterocycles;Matsakaici & Fine Chemicals;Pharmaceutical API.

Bayanin Tsaro:

Bayanan Tsaro: S36/37

Bayanin Hatsari: R20/21/22

Lambobin haɗari: Xi

Lambar HS: 2933590090

Ajiye: An adana shi a cikin akwati mai sanyi kuma busasshiyar da aka rufe sosai.Ka nisanci danshi da haske mai ƙarfi / zafi.

Bayyanar:Farar ko kashe-fari crystalline foda

Assay:Ba kasa da 99%

Yawan yawa:1.39 / cm3

Fahimtar Filashi:353.675 ℃

Wurin tafasa:661.189 ℃

Wurin narkewa:202 ℃

Turi:0.0± 2.0 mmHg a 25 ° C

Aika mana imel

Cikakken Bayani

Tags samfurin

Bayanin Samfura

Sunan samfur	Linagliptin CAS NO668270-12-0
Makamantu	(R)-8-(3-aminopperidin-1-yl)-7-(amma-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H) -dione;
CAS No	668270-12-0
Tsarin kwayoyin halitta	Saukewa: C25H28N8O2
Nauyin Kwayoyin Halitta	472.542

Aikace-aikace

1. Linagliptin (BI-1356) shine mai hana DPP-4, wani enzyme wanda ke lalata incretin hormones glucagon-like peptide-1 (GLP-1) da insulinotropic polypeptide (GIP-dogaran 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 wani sabon labari ne mai ƙarfi kuma mai zaɓin dipeptidyl peptidase-4 (DPP-4) mai hanawa tare da yuwuwar amfani a cikin maganin ciwon sukari na 2.
Ma'aikatan masana'antar mu ta Linagliptin matsakaici CAS 3355-28-0, fasahar balagagge, ingantaccen fitarwa, tabbacin inganci.
Matsayin Inventory: A Stock.
Idan kuna sha'awar samfuranmu ko kuna da wasu tambayoyi, da fatan za ku iya tuntuɓar mu!
Ana ba da samfuran ƙarƙashin ikon mallaka don manufar R & D kawai.

Amfani: Yana da ƙarfi, mai hanawa DPP-4 mai zaɓi tare da ƙimar IC50 na 1 nM.
Nazarin in vitro: Ligagliptin ya hana ayyukan DPP-4 a cikin vitro a cikin gwaje-gwaje masu zaman kansu da yawa tare da ƙimar IC50 na 0.4,0.5,0.9 da 1.1nM (yana nufin IC50, kusan 1nM).IC50 na hanawar FAP ta liagliptin shine 89 nM (kimanin zaɓin ninka 90 dangane da DPP-4).
A cikin binciken vivo: A cikin berayen Wistar na maza, karnuka Beagle da birai rhesus, an nuna xanthine linagliptin yana da inganci, mai dorewa kuma mai hanawa DPP-4 tare da> 7 h> 70% / kg bayan 1 MG na maganin baka.Gudanar da baki na ritagliptin zuwa berayen db / db kadai, mintuna 45 kafin gwajin haƙuri na glucose na baka, dogaro da kashi ya rage canjin glucose na plasma daga 0.1mg / kg (hana 15%) zuwa 1mg / kg (hana 66%) [1] .Ligagliptin (3 da 10mg / kg) kashi-dogara ya hana enzyme DPP-4 a cikin plasma a cikin mintuna 30 na sarrafa magunguna.Ligagliptin (1 MG / kg, po) yana rage yawan raguwar glucose da kusan 50% [2].Gudanar da baka na DPP-4 inhibitor ligagliptin (3mg / kg, gudanarwar baka) yana da ƙarfi ya rage ayyukan DPP-4, daidaita GLP-1 mai aiki a cikin raunuka na yau da kullun, da ingantaccen warkarwa a cikin ƙwayoyin ob / ob.A rana ta 10 bayan raunin da ya faru, liagliptin-magani ob / ob mice sun nuna yawancin raunuka epithelialized, halin rashin neutrophils.
Takardun: An gano sabon nau'in sinadari na masu hana masu hana DPP-4 da aka samo asali daga xanthine scaffold don kula da nau'in ciwon sukari na 2 kuma an kimanta shi.Bambance-bambancen tsari na tsari sun haifar da 1 (BI 1356), mai ƙarfi mai ƙarfi, zaɓi, dogon aiki, da mai hana DPP-4 na baki wanda ke nuna raguwar glucose na jini a cikin nau'ikan dabbobi daban-daban.1 a halin yanzu yana jurewa gwajin lokaci IIb na asibiti kuma yana riƙe da yuwuwar magani sau ɗaya a rana na nau'in ciwon sukari na 2.

Na baya: (R)-3-(Boc-Amino) piperidine, (R)-(+) -3-tert-Butoxycarbonylaminoperidine

Na gaba: 1- (Piperidin-4-yl) -1H-imidazo [4,5-b] pyridin-2 (3H) - dihydrochloride daya.