Ticagrelor

Tsanangudzo Pfupi

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Ticagrelor Anticoagulant Mumba 28984  


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Background

Ticagrelor mutsigiri mutsva weP2Y12 receptor [1].

Ticagrelor yakanzi inhibisa maitiro eprothrombotic eADP paplatelet nekurwisana neP2Y12 receptor.Ticagrelor yakaratidza kuvharwa kwakakwana kweplatelet aggregation ex vivo.Mukuwedzera Ticagrelor yakaratidza kuvharidzirwa-kunotsamira kweplatelet aggregation mumunhu.Kunze kweizvi, Ticagrelor yakaratidzawo nemuromo, kushingaira, reversibly kusunga anopikisa.Kusiyana nemamwe inhibitors, Ticagrelor yakashumawo kuti inhibit P2Y12 receptor pasina metabolic shanduko.Kunze kweizvozvo, Ticagrelor ndiyo yekutanga thienopyridine anti-platelet agent uye inonyanya kushandiswa neCYP3A4 uye CYP2C19 [1][2].

References:
[1] Zhou D1, Andersson TB, Grimm SW.In vitro kuongororwa kwezvinogona kushandiswa kwezvinodhaka-zvinodhaka ne ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, uye differential kinetics.Drug Metab Dispos.2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW.Maitiro uye metabolism ye ticagrelor, inoveli P2Y12 receptor antagonist, mumakonzo, makonzo, uye marmosets.Drug Metab Dispos.2011 Sep;39(9):1555-67.doi: 10.1124/dmd.111.039669.Epub 2011 Jun 13.

Tsanangudzo

Ticagrelor (AZD6140) inopindurwa muromo weP2Y12 receptor antagonist yekurapa kweplatelet aggregation.

In Vitro

Ticagrelor inokurudzira kudziviswa kukuru kweadenosine 5'-diphosphate (ADP)-yakakonzera Ca2+ kuburitswa muished maplatelet vs vamwe P2Y12R vanopikisa.Iyi yakawedzera mhedzisiro yeticagrelor kupfuura P2Y12R antagonism iri muchikamu semhedzisiro yeticagrelor inhibiting equilibrative nucleoside transporter 1 (ENT1) pamaplatelet, zvichiita kuti kuunganidzwa kwe extracellular adenosine uye activation yeGs-coupled adenosine A2A receptors [1].B16-F10 masero anoratidza kuderera kwekubatana nemaplatelet kubva kune ticagrelor-treated mice kana ichienzaniswa nesaline-treated mice [2].

MuB16-F10 melanoma intravenous uye intrasplenic metastasis mienzaniso, mice inobatwa nekiriniki yeticagrelor (10 mg / kg) inoratidza kuderedzwa kwemapapu (84%) uye chiropa (86%) metastases.Uyezve, kurapwa kweticagrelor kunovandudza kupona kana kuenzaniswa nemhuka dzine saline.Chiitiko chakafanana chinoonekwa mumuenzaniso wekenza yemazamu ye4T1, nekuderedza mumapapu (55%) uye bone marrow (87%) metastases inotevera ticagrelor kurapwa [2].Single oral administration ye ticagrelor (1-10 mg / kg) inokonzera dose-yakabatana inhibitory effect pa platelet aggregation.Ticagrelor, pamwero wepamusoro (10 mg / kg) inodzivisa zvakanyanya kusanganiswa kweplatelet pa 1 h mushure mekuita dosing uye peak inhibition inoonekwa pa4 h mushure mekuita dosing.

Storage

4°C, kudzivirira kubva kuchiedza, kuchengetwa pasi penitrogen

*In solvent : -80°C, mwedzi mitanhatu;-20°C, mwedzi 1 (dzivirira kubva kuchiedza, yakachengetwa pasi penitrogen)

Chimiro chemakemikari

Ticagrelor

CERTIFICATE

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

HUNHU MANAGEMENT

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Quality management4

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