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

sharaxaad gaaban:

Kiimikada & Qalabka Jirka

Qaybta: Qalabka ceeriin ee daawada;Kahortagayaasha;Amines;Aromatics; Heterocycles; Dhexdhexaadiyaha & Kiimikada Fiican;Pharmaceutical API.

Macluumaadka Badbaadada:

Bayaanada Badbaadada: S36/37

Bayaanada halista: R20/21/22

Koodhadhka halista: Xi

HS code: 2933590090

Kaydinta: Waxaa lagu kaydiyaa weel qabow oo engegan oo si fiican u xidhan.Ka fogow qoyaanka iyo iftiinka/kulka xooggan.

Muuqashada:Budada crystalline cad ama ka baxsan

Qiimayn:Wax ka yar 99%

Cufnaanta:1.39/cm3

Barta Tooshka ah:353.675 ℃

Barta Karkari:661.189 ℃

Barta dhalaalka:202℃

Cadaadis uumiga:0.0±2.0 mmHg at 25°C

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Faahfaahinta Alaabta

Tags Product

Sharaxaada Alaabta

Magaca Alaabta	Linagliptin CAS NO668270-12-0
La mid ah	(R)-8-(3-aminopperidin-1-yl)-7-(laakin-2-yn-1-yl)-3-Methyl-1-((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione;
CAS Maya	668270-12-0
Qaanuunka molecular	C25H28N8O2
Miisaanka Molecular	472.542

Codsiga

1. Linagliptin (BI-1356) waa horjooge DPP-4, ensaymes oo hoos u dhiga hormoonnada glucagon-sida peptide-1 (GLP-1) iyo gulukoos-ku-tiirsan 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 waa awood cusub oo awood leh oo door ah dipeptidyl peptidase-4 (DPP-4) inhibitor oo leh isticmaalka suurtagalka ah ee daaweynta nooca 2aad ee sonkorowga.
Warshadayadu waxay soo saartaa Linagliptin dhexdhexaadka ah CAS 3355-28-0, tignoolajiyada qaan-gaadhka ah, wax soo saarka xasilloon, hubinta tayada.
Xaalada Alaabada : Kaydka
Haddii aad xiisaynayso alaabtayada ama aad qabto wax su'aalo ah, fadlan xor u noqo inaad nala soo xidhiidho!
Alaabooyinka hoos yimaada patentka waxaa loo bixiyaa ujeeddooyin R & D oo keliya.

Isticmaal: Waa wax-qabad awood leh, doorta DPP-4 oo leh IC50 qiime ah 1 nM.
Daraasadda gudaha: Ligagliptin waxay joojisay dhaqdhaqaaqa DPP-4 gudaha vitro dhowr tijaabo oo madax-bannaan oo leh IC50 qiimaha 0.4,0.5,0.9 iyo 1.1nM (macnaha IC50, qiyaastii 1nM).IC50 ee joojinta FAP ee liagliptin waxay ahayd 89 nM (qiyaastii 90-laab xulashada marka loo eego DPP-4).
In vivo cilmi-baarista: Rajada Wistar ee ragga, eyda Beagle iyo daayeerrada rhesus, xanthine linagliptin waxaa lagu muujiyay inuu yahay mid wax ku ool ah, waara oo awood leh DPP-4 inhibitor leh> 7 h> 70% / kg ka dib 1 mg oo maamulka afka ah.Maamulka afka ee ritagliptin ilaa jiirarka db / db keligiis, 45 min ka hor tijaabada dulqaadka gulukooska afka, qiyaasta ku-tiirsanaanta waxay hoos u dhigtay isbeddelka gulukooska balaasmaha 0.1mg / kg (15% xannibaad) ilaa 1mg / kg (66% xannibaad) [1] .Ligagliptin (3 iyo 10mg / kg) qiyaasta-ku-tiirsanaanta waxay hakisay enzyme DPP-4 ee balaasmaha 30 daqiiqo gudahood maamulka daroogada.Ligagliptin (1 mg / kg, po) waxay si weyn hoos ugu dhigtay heerka sonkorta dhiigga 50% [2].Maamulka afka ee DPP-4 inhibitor ligagliptin (3mg / kg, maamulka afka) ayaa si xoog leh hoos u dhigay dhaqdhaqaaqa DPP-4, xasilinta firfircoon ee GLP-1 ee nabarrada dabadheeraad ah, iyo bogsashada wanaajinta jiirarka ob / ob.Maalintii 10-aad dhaawaca ka dib, jiirarka la daaweeyay ee liagliptin waxay muujiyeen nabarrada epithelialized inta badan, oo lagu garto maqnaanshaha neutrophils.
Dukumeenti: Nooc cusub oo kiimiko ah oo ah horjoogayaasha awooda DPP-4 oo qaab dhismeed ka soo jeeda xanthine scaffold ee daaweynta nooca 2 ee sonkorowga ayaa la helay oo la qiimeeyay.Kala duwanaanshiyaha qaabdhismeedka habaysan ayaa keenay 1 (BI 1356), oo ah mid aad u awood badan, door ah, dhaq-dhaqaaq dheer, iyo inhibitor DPP-4 oo afka ah oo muujinaya hoos u dhac weyn oo gulukoos dhiig ah oo ku jira noocyada kala duwan ee xayawaanka.1 wuxuu hadda ku socdaa tijaabooyinka wajiga IIb ee kiliinikada wuxuuna hayaa suurtagalnimada daawaynta hal mar maalinlaha ah ee nooca 2 ee sonkorowga.

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

Xiga: 1-(Piperidin-4-yl)-1H-imidazo[4,5-b]pyridin-2(3H) -hal dihydrochloride