SGLT1/2

KATSE # Lebitso la Sehlahiswa Tlhaloso
CPD100587 Philorizin Phlorizin, eo hape e bitsoang phloridzin, ke glucoside ea phloretin, dihydrochalcone, lelapa la bicyclic flavonoids, eo hape e leng sehlotšoana sa mefuta e fapaneng ea phenylpropanoid synthesis ea limela. Phlorizin ke inhibitor ea tlhōlisano ea SGLT1 le SGLT2 hobane e hlōlisana le D-glucose bakeng sa ho tlama ho mojari; Sena se fokotsa ho tsamaisoa ha tsoekere ea renal, ho theola bongata ba tsoekere maling. Phlorizin e ile ea ithutoa e le pheko e ka bang teng ea meriana bakeng sa lefu la tsoekere la mofuta oa 2, empa haesale e nkeloa sebaka ke li-analogue tsa maiketsetso tse ikhethileng, tse kang canagliflozin le dapagliflozin.
CPD0045 Ipragliflozin Ipragliflozin, eo hape e tsejoang e le ASP1941, ke inhibitor e matla le e khethang ea SGLT2 bakeng sa kalafo ea lefu la tsoekere la mofuta oa 2. Phekolo ea Ipragliflozin e ntlafalitse taolo ea glycemic ha e eketsoa kalafong ea metformin mme e ka amahanngoa le ho theola boima ba 'mele le phokotso ea khatello ea mali ha e bapisoa le placebo. Ipragliflozin ha e ntlafatse hyperglycemia feela empa hape le lefu la tsoekere / botenya bo amanang le metabolic litoeba tsa mofuta oa 2 oa lefu la tsoekere. E ile ea amoheloa hore e sebelisoe Japane ka 2014
CPD100585 Tofogliflozin Tofogliflozin, eo hape e tsejoang e le CSG 452, ke inhibitor e matla le e khethang haholo ea SGLT2 e ntseng e tsoela pele kalafong ea lefu la tsoekere. Tofogliflozin e ntlafatsa taolo ea glycemic le ho theola boima ba 'mele ho bakuli ba nang le lefu la tsoekere la mofuta oa 2. Tofogliflozin e hatella ho kenella ha tsoekere ka har'a lisele tsa tubula e itšetlehileng ka tekanyetso. Ho pepeseha ha tsoekere e phahameng (30?mM) bakeng sa 4 le 24?h ho ile ha eketsa haholo tlhahiso ea khatello ea oxidative liseleng tsa tubular, tse neng li hatelloa ke kalafo ea tofogliflozin kapa antioxidant N-acetylcysteine ​​(NAC).
CPD100583 Empagliflozin Empagliflozin, e tsejoang hape e le BI10773 (lebitso la khoebo la Jardiance), ke moriana o amohetsoeng bakeng sa ho alafa lefu la tsoekere la mofuta oa 2 ho batho ba baholo ka 2014. E entsoe ke Boehringer Ingelheim le Eli Lilly and Company. Empagliflozin ke inhibitor ea sodium glucose co-transporter-2 (SGLT-2), mme e etsa hore tsoekere e maling e monoe ke liphio ebe e ntšoa ka moroto. Empagliflozin ke inhibitor ea sodium glucose co-transporter-2 (SGLT-2), e fumanehang feela ka har'a li-proximal tubules tsa likarolo tsa nephronic liphio. SGLT-2 e etsa karolo ea 90 lekholong ea ho kenngoa ha tsoekere maling.
CPD100582 Canagliflozin Canagliflozin (INN, lebitso la khoebo Invokana) ke setlhare sa kalafo ea lefu la tsoekere la mofuta oa 2. E entsoe ke Mitsubishi Tanabe Pharma 'me e rekisoa tlas'a laesense ke Janssen, karolo ea Johnson & Johnson. Canagliflozin ke inhibitor ea subtype 2 sodium-glucose transport protein (SGLT2), e ikarabellang bonyane 90% ea ho kenngoa ha tsoekere ka liphio. Ho thibela sepalangoang sena ho etsa hore tsoekere ea mali e tsoe ka moroto. Ka Hlakubele 2013, canagliflozin e bile inhibitor ea pele ea SGLT2 ho amoheloa United States.
CPD0003 Dapagliflozin Dapagliflozin, eo hape e tsejoang e le BMS-512148, ke setlhare se sebelisoang ho alafa lefu la tsoekere la mofuta oa 2 se amohetsoeng ka 2012 ke FDA. Dapagliflozin e thibela mofuta oa 2 oa liprotheine tse tsamaisang tsoekere ea sodium (SGLT2) tse ikarabellang bonyane 90% ea ho kenngoa ha tsoekere ka liphio. Ho thibela mochine ona oa lipalangoang ho etsa hore tsoekere ea mali e tlosoe ka moroto. Litekong tsa bongaka, dapagliflozin e theotse HbA1c ka 0.6 ha e bapisoa le karolo ea placebo ha e kenngoa ho metformin.
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