SGLT1/2

IKATI # Igama Lomkhiqizo Incazelo
I-CPD100587 I-Phlorizin I-Phlorizin, ebizwa nangokuthi i-phloridzin, iyi-glucoside ye-phloretin, i-dihydrochalcone, umndeni wama-bicyclic flavonoids, nawo abe yiqembu elincane elisendleleni eyahlukene ye-phenylpropanoid synthesis ezitshalweni. I-Phlorizin iyi-inhibitor eqhudelanayo ye-SGLT1 ne-SGLT2 ngoba iqhudelana ne-D-glucose ukuze ibophezele kusiphathi; lokhu kunciphisa ukuthuthwa kwe-glucose ezinso, kwehlisa inani le-glucose egazini. I-Phlorizin yacwaningwa njengendlela yokwelapha engaba yimithi yohlobo 2 lwesifo sikashukela, kodwa kusukela ngaleso sikhathi isithathelwe indawo ngama-analogue okwenziwa athembisayo, njenge-canagliflozin ne-dapagliflozin.
CPD0045 I-Ipragliflozin I-Ipragliflozin, eyaziwa nangokuthi i-ASP1941, iyisivimbeli se-SGLT2 esinamandla futhi esikhethayo ekwelapheni uhlobo 2 sikashukela. Ukwelashwa kwe-Ipragliflozin kuthuthukise ukulawulwa kwe-glycemic lapho yengezwa ekwelashweni kwe-metformin futhi kungahlotshaniswa nokuncipha kwesisindo kanye nokuncipha komfutho wegazi uma kuqhathaniswa ne-placebo. I-Ipragliflozin ayithuthukisi i-hyperglycemia kuphela kodwa futhi nesifo sikashukela/ukukhuluphala okuhlobene nokungajwayelekile kwe-metabolic kumagundane ohlobo 2 lwesifo sikashukela. Yavunywa ukuthi isetshenziswe e-Japan ngo-2014
I-CPD100585 I-Tofogliflozin I-Tofogliflozin, eyaziwa nangokuthi i-CSG 452, iyi-inhibitor enamandla futhi ekhetha kakhulu ye-SGLT2 ngaphansi kokuthuthukiswa kokwelashwa kwesifo sikashukela. I-Tofogliflozin ithuthukisa ukulawulwa kwe-glycemic futhi yehlise isisindo somzimba ezigulini ezinesifo sikashukela sohlobo 2. I-Tofogliflozin incike kumthamo we-glucose ukungena kumaseli we-tubular. Ukuchayeka kwe-glucose ephezulu (30?mM) ku-4 kanye no-24?h kwandise kakhulu ukukhiqizwa kwengcindezi ye-oxidative kumaseli e-tubular, ayecindezelwe ukwelashwa kwe-tofogliflozin noma i-antioxidant N-acetylcysteine ​​(NAC).
I-CPD100583 I-Empagliflozin I-Empagliflozin, eyaziwa nangokuthi i-BI10773 (igama lokuhweba elithi Jardiance), iyisidakamizwa esigunyazwe ukwelapha isifo sikashukela sohlobo 2 kubantu abadala ngo-2014. Yasungulwa ngu-Boehringer Ingelheim no-Eli Lilly and Company. I-Empagliflozin iyi-inhibitor ye-sodium glucose co-transporter-2 (SGLT-2), futhi ibangela ukuthi ushukela osegazini udonswe yizinso futhi uphume emchamweni. I-Empagliflozin iyi-inhibitor ye-sodium glucose co-transporter-2 (SGLT-2), etholakala cishe kuphela kuma-proximal tubules wezingxenye ze-nephronic ezinso. I-SGLT-2 ilandisa cishe ngamaphesenti angama-90 wokufakwa kabusha kweglucose egazini.
I-CPD100582 I-Canagliflozin I-Canagliflozin (INN, igama lokuhweba i-Invokana) umuthi wokwelapha uhlobo 2 sikashukela. Yasungulwa ngabakwaMitsubishi Tanabe Pharma futhi imakethwa ngaphansi kwelayisensi ngu-Janssen, ingxenye ye-Johnson & Johnson. I-Canagliflozin iyi-inhibitor ye-subtype 2 ye-sodium-glucose transport protein (SGLT2), enesibopho okungenani esingu-90% sokumuncwa kabusha kwe-glucose ezinso. Ukuvimba lesi sithuthi kubangela ukuthi i-glucose yegazi iphume ngomchamo. NgoMashi 2013, i-canagliflozin yaba inhibitor yokuqala ye-SGLT2 ukugunyazwa e-United States.
CPD0003 I-Dapagliflozin I-Dapagliflozin, eyaziwa nangokuthi i-BMS-512148, umuthi osetshenziselwa ukwelapha isifo sikashukela sohlobo 2 owagunyazwa yi-FDA ngo-2012. I-Dapagliflozin ivimbela i-subtype 2 yamaprotheni ezokuthutha i-sodium-glucose (SGLT2) abangela okungenani u-90% wokumuncwa kabusha kwe-glucose ezinso. Ukuvimbela le nqubo ye-transporter kubangela ukuthi i-glucose yegazi ikhishwe ngomchamo. Ezivivinyweni zomtholampilo, i-dapagliflozin yehlise i-HbA1c ngamaphuzu angu-0.6 uma iqhathaniswa namaphesenti e-placebo lapho ingezwa ku-metformin.
...
Ingxoxo ye-WhatsApp Online!