SGLT1/2

MPAKA # Dzina lazogulitsa Kufotokozera
CPD100587 Phlorizin Phlorizin, yomwe imatchedwanso phloridzin, ndi glucoside wa phloretin, dihydrochalcone, banja la bicyclic flavonoids, lomwe liri kagulu kakang'ono mumitundu yosiyanasiyana ya phenylpropanoid synthesis pathway mu zomera. Phlorizin ndi mpikisano woletsa SGLT1 ndi SGLT2 chifukwa amapikisana ndi D-glucose kuti amangirire kwa chonyamulira; izi zimachepetsa kayendedwe ka shuga wa aimpso, kutsitsa kuchuluka kwa shuga m'magazi. Phlorizin idaphunziridwa ngati mankhwala otheka amtundu wa 2 shuga, koma kuyambira pamenepo idasinthidwa ndi ma analogi opangira okhazikika, monga canagliflozin ndi dapagliflozin.
Chithunzi cha CPD0045 Ipragliflozin Ipragliflozin, yomwe imadziwikanso kuti ASP1941, ndiyoletsa komanso yosankha SGLT2 inhibitor pochiza matenda amtundu wa 2. Chithandizo cha Ipragliflozin chimawongolera kuwongolera kwa glycemic mukaphatikizidwa ndi metformin ndipo kumatha kulumikizidwa ndi kuchepa thupi komanso kuchepa kwa kuthamanga kwa magazi poyerekeza ndi placebo. Ipragliflozin sikuti imangowonjezera hyperglycemia komanso matenda a shuga / kunenepa kwambiri okhudzana ndi zovuta za metabolic mumtundu wa 2 matenda a shuga. Inavomerezedwa kuti igwiritsidwe ntchito ku Japan mu 2014
CPD100585 Tofogliflozin Tofogliflozin, yomwe imadziwikanso kuti CSG 452, ndiyomwe inhibitor yamphamvu komanso yosankha kwambiri ya SGLT2 yomwe imapangidwa pochiza matenda a shuga. Tofogliflozin imathandizira kuwongolera glycemic ndikuchepetsa kulemera kwa odwala omwe ali ndi matenda amtundu wa 2. Tofogliflozin amadalira mlingo wa glucose kulowa m'maselo a tubular. Kuwonetsa shuga wambiri (30?mM) kwa 4 ndi 24?h kunachulukitsa kwambiri kupsinjika kwa okosijeni m'maselo a tubular, omwe adatsitsidwa ndi chithandizo cha tofogliflozin kapena antioxidant N-acetylcysteine ​​(NAC).
CPD100583 Empagliflozin Empagliflozin, yomwe imadziwikanso kuti BI10773 (dzina la malonda Jardiance), ndi mankhwala ovomerezeka kuti azichiza matenda a shuga amtundu wa 2 mwa akuluakulu mu 2014. Anapangidwa ndi Boehringer Ingelheim ndi Eli Lilly and Company. Empagliflozin ndi inhibitor ya sodium glucose co-transporter-2 (SGLT-2), ndipo imapangitsa kuti shuga m'magazi atengeke ndi impso ndikuchotsedwa mumkodzo. Empagliflozin ndi choletsa cha sodium glucose co-transporter-2 (SGLT-2), yomwe imapezeka pafupifupi m'ma proximal tubules a zigawo za nephronic mu impso. SGLT-2 imapanga pafupifupi 90 peresenti ya glucose reabsorption m'magazi.
CPD100582 Mankhwala a canagliflozin Canagliflozin (INN, dzina la malonda Invokana) ndi mankhwala ochizira matenda amtundu wa 2. Idapangidwa ndi Mitsubishi Tanabe Pharma ndipo imagulitsidwa pansi pa chilolezo ndi Janssen, gawo la Johnson & Johnson. Canagliflozin ndi inhibitor ya subtype 2 sodium-glucose transport protein (SGLT2), yomwe imayang'anira pafupifupi 90% ya glucose reabsorption mu impso. Kuletsa chotengera ichi kumapangitsa kuti shuga wamagazi achotsedwe kudzera mumkodzo. Mu Marichi 2013, canagliflozin idakhala inhibitor yoyamba ya SGLT2 kuvomerezedwa ku United States.
CPD0003 Dapagliflozin Dapagliflozin, yomwe imadziwikanso kuti BMS-512148, ndi mankhwala omwe amagwiritsidwa ntchito pochiza matenda a shuga a 2 omwe adavomerezedwa mu 2012 ndi FDA. Dapagliflozin imalepheretsa subtype 2 ya mapuloteni a sodium-glucose transport (SGLT2) omwe amayang'anira pafupifupi 90% ya glucose reabsorption mu impso. Kuletsa njira yonyamula iyi kumapangitsa kuti shuga wamagazi achotsedwe kudzera mumkodzo. M'mayesero azachipatala, dapagliflozin idatsitsa HbA1c ndi 0.6 poyerekeza ndi gawo la placebo ikawonjezeredwa ku metformin.
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