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

Linagliptin;8-[(3R) -3-aminoperidin-1-yl] -7-sugbon-2-ynyl-3-methyl-1-[(4-methylquinazolin-2-yl) methyl] purine-2,6-dione Ti a ṣe afihan Aworan

kukuru apejuwe:

Kemikali & Ti ara Properties

Ẹka: Awọn ohun elo elegbogi;Inhibitor;Amines;Aromatics;Heterocycles;Intermediates & Fine Kemikali;Elegbogi API.

Alaye Abo:

Awọn Gbólóhùn Abo: S36/37

Ewu Gbólóhùn: R20/21/22

Awọn koodu ewu: Xi

HS koodu: 2933590090

Ibi ipamọ: Ti a fipamọ sinu apo ti o tutu ati gbẹ daradara.Jeki kuro lati ọrinrin ati ina to lagbara / ooru.

Irisi:Funfun tabi pa-funfun okuta lulú

Ayẹwo:Ko kere ju 99%

Ìwúwo:1,39 / cm3

Oju filaṣi:353.675 ℃

Oju Ise:661.189 ℃

Ibi yo:202℃

Ipa oru:0.0±2.0 mmHg ni 25°C

Fi imeeli ranṣẹ si wa

Alaye ọja

ọja Tags

ọja Apejuwe

Orukọ ọja	Linagliptin CAS NO668270-12-0
Awọn itumọ ọrọ sisọ	(R) -8- (3-aminoperidin-1-yl) -7- (ṣugbọn-2-yn-1-yl) -3-Methyl-1- ((4-Methylquinazolin-2-yl) Methyl) -1H -purine-2,6 (3H,7H) -dione;
CAS No	668270-12-0
Ilana molikula	C25H28N8O2
Òṣuwọn Molikula	472.542

Ohun elo

1. Linagliptin (BI-1356) jẹ inhibitor ti DPP-4, enzymu kan ti o dinku awọn homonu incretin glucagon-like peptide-1 (GLP-1) ati glukosi ti o gbẹkẹle 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 jẹ aramada ti o lagbara ati ti o yan dipeptidyl peptidase-4 (DPP-4) inhibitor pẹlu lilo agbara ni itọju iru àtọgbẹ 2.
Ile-iṣẹ iṣelọpọ wa ti Linagliptin agbedemeji CAS 3355-28-0, imọ-ẹrọ ti ogbo, iṣelọpọ iduroṣinṣin, idaniloju didara.
Ipo Iṣura: Ninu Iṣura.
Ti o ba nifẹ si awọn ọja wa tabi ni ibeere eyikeyi, jọwọ lero ọfẹ lati kan si wa!
Awọn ọja labẹ itọsi wa fun idi R&D nikan.

Lo: O jẹ oludaniloju DPP-4 ti o lagbara, ti o yan pẹlu iye IC50 ti 1 nM.
Iwadi in vitro: Ligagliptin ṣe idiwọ iṣẹ DPP-4 ni fitiro ni ọpọlọpọ awọn adanwo ominira pẹlu awọn iye IC50 ti 0.4,0.5,0.9 ati 1.1nM (tumọ si IC50, isunmọ 1nM).IC50 ti idinamọ FAP nipasẹ liagliptin jẹ 89 nM (nipa 90-fold selectivity ni ibatan si DPP-4).
Ninu iwadi vivo: Ninu awọn eku Wistar ọkunrin, awọn aja Beagle ati awọn obo rhesus, xanthine linagliptin ni a fihan lati jẹ imunadoko, ti o tọ ati agbara DPP-4 inhibitor pẹlu> 7 h> 70% / kg lẹhin 1 miligiramu ti iṣakoso ẹnu.Isakoso ẹnu ti ritagliptin si awọn eku db / db nikan, awọn iṣẹju 45 ṣaaju idanwo ifarada glukosi ẹnu, ni igbẹkẹle iwọn lilo dinku iyipada glukosi pilasima lati 0.1mg / kg (idinamọ 15%) si 1mg / kg (idinamọ 66%) [1] .Ligagliptin (3 ati 10 miligiramu / kg) ni igbẹkẹle-igbẹkẹle ṣe idiwọ henensiamu DPP-4 ninu pilasima laarin awọn iṣẹju 30 ti iṣakoso oogun.Ligagliptin (1 miligiramu / kg, po) dinku aiṣedeede glukosi ni pataki nipasẹ iwọn 50% [2].Isakoso ẹnu ti DPP-4 inhibitor ligagliptin (3mg / kg, iṣakoso ẹnu) dinku iṣẹ ṣiṣe DPP-4 ni agbara, muduro GLP-1 lọwọ ni awọn ọgbẹ onibaje, ati ilọsiwaju imularada ni awọn eku ob / ob.Ni ọjọ 10 lẹhin ọgbẹ, awọn eku ob / ob ti a ṣe itọju liagliptin fihan pupọ julọ awọn ọgbẹ epithelialized, ti a fihan nipasẹ isansa ti neutrophils.
Iwe-ipamọ: Kilasi kẹmika tuntun ti awọn inhibitors DPP-4 ti o lagbara ti a mu ni igbekale lati inu xanthine scaffold fun itọju iru àtọgbẹ 2 ni a ti ṣe awari ati ṣe iṣiro.Awọn iyatọ igbekalẹ eleto ti yori si 1 (BI 1356), ti o lagbara pupọ, yiyan, ṣiṣe pipẹ, ati inhibitor DPP-4 ti n ṣiṣẹ ni ẹnu ti o ṣe afihan idinku glukosi ẹjẹ pupọ ni awọn oriṣiriṣi ẹranko.1 lọwọlọwọ n gba awọn idanwo ile-iwosan alakoso IIb ati pe o ni agbara fun itọju lẹẹkan lojoojumọ ti iru awọn alakan 2.

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

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