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

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Chemical & Physical Properties

Qeb: Pharmaceutical raw khoom;Inhibitor; Amines; Aromatics; Heterocycles; Intermediates & Fine Chemicals;Pharmaceutical API.

Cov ntaub ntawv kev nyab xeeb:

Cov Lus Qhia Txog Kev Nyab Xeeb: S36/37

Risk Nqe: R20/21/22

Hazard Codes: Xis

HS Code: 2933590090

Cia: Khaws rau hauv lub thawv txias thiab qhuav zoo kaw.Khaws kom deb ntawm noo noo thiab lub teeb muaj zog / tshav kub.

Qhov tsos:Dawb los yog tawm-dawb crystalline hmoov

Assay:Tsis pub tsawg tshaj 99%

Ceev:1.39 / cm3

Flash Point:353.675 ℃

Boiling Point:661.189 ℃

Melting point:202 ℃

Vapor Pressure:0.0 ± 2.0 mmHg ntawm 25 ° C

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Product Detail

Khoom cim npe

Product Description

Khoom npe	Linagliptin CAS NO 668270-12-0
Synonyms	(R)-8-(3-aminopiperidin-1-yl)-7-(tab sis-2-yn-1-yl)-3-Methyl-1-(((4-Methylquinazolin-2-yl)Methyl)-1H -purine-2,6(3H,7H)-dione;
CAS Nr	668270-12-0
Molecular Formula	C25H28N8O2
Molecular Luj	472.542 ib

Daim ntawv thov

1. Linagliptin (BI-1356) yog ib qho inhibitor ntawm DPP-4, ib qho enzyme uas degrades incretin hormones glucagon-zoo li peptide-1 (GLP-1) thiab qabzib-dependent 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 yog ib qho tshiab muaj zog thiab xaiv dipeptidyl peptidase-4 (DPP-4) inhibitor uas muaj peev xwm siv tau hauv kev kho mob ntshav qab zib hom 2.
Peb lub Hoobkas tsim cov Linagliptin intermediate CAS 3355-28-0, mature technology, ruaj khov tso zis, kev ruaj ntseg zoo.
Inventory Status: Hauv Tshuag.
Yog tias koj txaus siab rau peb cov khoom lossis muaj lus nug, thov koj xav tiv tauj peb!
Cov khoom raws li patent yog muab rau R & D lub hom phiaj nkaus xwb.

Siv: Nws yog lub zog, xaiv DPP-4 inhibitor nrog IC50 tus nqi ntawm 1 nM.
Kev tshawb fawb hauv vitro: Ligagliptin inhibited DPP-4 kev ua hauv vitro hauv ntau qhov kev sim ywj pheej nrog IC50 qhov tseem ceeb ntawm 0.4,0.5,0.9 thiab 1.1nM (txhais tau tias IC50, kwv yees li 1nM).IC50 ntawm FAP inhibition los ntawm liagliptin yog 89 nM (kwv yees 90-fold selectivity txheeb ze rau DPP-4).
Hauv kev tshawb fawb vivo: Hauv cov txiv neej Wistar nas, Beagle dev thiab rhesus liab, xanthine linagliptin tau pom tias yog qhov ua tau zoo, ruaj khov thiab muaj zog DPP-4 inhibitor nrog> 7 h> 70% / kg tom qab 1 mg ntawm kev tswj qhov ncauj.Kev tswj hwm ntawm qhov ncauj ntawm ritagliptin rau db / db nas ib leeg, 45 feeb ua ntej qhov ntsuas qhov ncauj qhov siab, koob tshuaj txo qis hauv cov ntshav qabzib hloov ntawm 0.1mg / kg (15% inhibition) mus rau 1mg / kg (66% inhibition) [1] .Ligagliptin (3 thiab 10mg / kg) koob tshuaj-raws li inhibited DPP-4 enzyme hauv cov ntshav hauv 30 feeb ntawm kev tswj hwm tshuaj.Ligagliptin (1 mg / kg, po) txo cov piam thaj ntau li 50% [2].Kev tswj qhov ncauj ntawm DPP-4 inhibitor ligagliptin (3mg / kg, kev tswj qhov ncauj) txo qis DPP-4 kev ua haujlwm, ua kom muaj zog ntawm GLP-1 hauv cov qhov txhab mob, thiab txhim kho kev kho mob hauv ob / ob nas.Nyob rau hnub 10 tom qab raug mob, liagliptin-kho ob / ob nas pom feem ntau cov kab mob epithelialized, tus cwj pwm los ntawm qhov tsis muaj neutrophils.
Cov ntaub ntawv: Cov chav kawm tshuaj tshiab ntawm cov muaj zog DPP-4 inhibitors tau tsim los ntawm xanthine scaffold rau kev kho mob ntshav qab zib hom 2 tau tshawb pom thiab tshuaj xyuas.Cov txheej txheem kev hloov pauv tau ua rau 1 (BI 1356), muaj zog heev, xaiv, ua haujlwm ntev, thiab qhov ncauj nquag DPP-4 inhibitor uas qhia tau hais tias cov ntshav qabzib ntau hauv cov tsiaj sib txawv.1 tam sim no tab tom tab tom kuaj xyuas theem IIb kev sim thiab tuav lub peev xwm rau kev kho mob ib hnub ib zaug ntawm cov neeg mob ntshav qab zib hom 2.

Yav dhau los: (R)-3-(Boc-Amino)piperidine, (R)-(+)-3-tert-Butoxycarbonylaminopiperidine

Tom ntej: 1-(Piperidin-4-yl)-1H-imidazo[4,5-b]pyridin-2(3H)-ib dihydrochloride