Inombolo ye-Cetilistat Cas: 282526-98-1 I-Molecular Formula:C25H39NO3
I-Melting Point | 72.0 kuya ku-76.0 °C |
Ukuminyana | 1.02 |
izinga lokushisa lokugcina | Ivalwe endaweni eyomile, engu-2-8°C |
ukuncibilika | I-Chloroform (Kancane), i-Ethyl Acetate (Kancane) |
umsebenzi optical | N/A |
Ukubukeka | I-Cryst Emhlophe |
Ubumsulwa | ≥98% |
I-Cetilistat (eyaziwa nangokuthi i-ATL-962) yagunyazwa ngoSepthemba 2013 nguMnyango Wezempilo, Wezabasebenzi Nenhlalakahle YaseJapan ukuze kwelashwe ukukhuluphala, kukhawulelwe ezigulini ezinakho kokubili uhlobo 2 lwesifo sikashukela i-mellitus (T2DM) kanye ne-dyslipidemia, kanye nesisindo somzimba. inkomba (BMI)25 kg/m2naphezu kokwelashwa ngokudla kanye/noma ukuvivinya umzimba.Njenge-orlistat, i-cetilistat isebenza ngokuvinjwa kwe-pancreatic lipase emathunjini ukuze ivimbele ukumuncwa kwamafutha futhi ngaleyo ndlela inciphise ukumuncwa kwekhalori ekudleni.Uhlelo lwekhemikhali yezokwelapha aluzange luchazwe ezincwadini zesayensi, kodwa ilungelo lobunikazi elichaza i-cetilistat liphinde lichaze ukuhlanganiswa kwama-analogue anama-aryl substituent ahlukahlukene kanye nemisila ye-lipophilic.Ukuhlanganiswa kwe-cetilistat kuhilela ukufingqa kwe-hexadecylcarbonochloridate nge-2-amino-5-methylbenzoic acid;amanye ama-analogue ahlanganiswa ngokuhlukahluka kwe-carbonochloridate kanye nezingxenye ze-2-aminobenzoic acid.I-Cetilistat iyi-inhibitor enamandla ye-pancreatic lipase yomuntu negundane ene-IC50sye-15 kanye ne-136 nM, ngokulandelana, ngokuvinjelwa okuncane kwe-trypsin noma i-chymotrypsin.
Inoveli ye-pancreatic lipase inhibitor yokwelashwa kokukhuluphala kuzo zombili iziguli ezinesifo sikashukela nezingezona ezinesifo sikashukela.
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