| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100573 | PF-05175157 | PF-05175157 ke inhibitor e matla le e khethang ea bobeli ba acetyl-CoA carboxylase isoform ACC1 e fumanehang haholo-holo ka har'a sebete le lisele tsa adipose le isoform ACC2 e laolang mesifa ea masapo le pelo, e nang le IC50 boleng ba 27 nM le 33 nM, ka ho latellana. ACC inhibitors inhibit de novo lipogenesis le ho eketsa β-oxidation ea li-acid tse telele tse nang le monyetla oa ho phekola lefu la tsoekere la mofuta oa 2, hepatic steatosis le mofets'e. |
| CPD100572 | ND-646 | ND-646 ke-allosteric inhibitor ea li-enzyme tsa ACC ACC1 le ACC2 tse thibelang ACC subunit dimerization-ho hatella motsoako oa acid e mafura ka hare ho vitro le vivo. Phekolo e sa foleng ea ND-646 ea xenograft le mefuta ea litoeba tse entsoeng ka liphatsa tsa lefutso tsa NSCLC e thibetse ho hola ha hlahala. Ha e sebelisoa e le moemeli a le mong kapa hammoho le sethethefatsi se tloaelehileng sa carboplatin, ND-646 e ile ea hatella kholo ea hlahala ea matšoafo ka mokhoa o hlakileng Kras; Trp53-/- (e tsejoang hape e le KRAS p53) le Kras; Stk11-/- ( e tsejoang hape e le KRAS Lkb1) mefuta ea litoeba ea NSCLC. ND-646 e ne e ntlafalitse ts'ebetso ha e kopantsoe le carboplatin, e leng karolo e tloaelehileng ea li-chemotherapeutic regimens tse sebelisetsoang ho phekola NSCLC ea motho. |
| CPD100571 | CP-640186 | CP-640186 ke inhibitor e matla ea mammalian ACCs 'me e ka fokotsa boima ba' mele le ho ntlafatsa kutloisiso ea insulin ho liphoofolo tsa liteko. CP-640186 e sa tsoa bontšoa e le inhibitor e matla ea li-isoforms tsa mammalian ACCs tse nang le boleng ba IC50 ba hoo e ka bang 55 nM. Hona joale ke eona feela inhibitor e matla e tlalehiloeng ea mammalian ACCs. Litloaelong tsa lisele hammoho le mehlala ea liphoofolo, CP-640186 e ka fokotsa litekanyetso tsa malonyl-CoA, ea thibela mafura a acid biosynthesis, 'me ea susumetsa mafura a acid oxidation. Habohlokoa ka ho fetesisa, CP-640186 e ka fokotsa boima ba 'mele le boima ba' mele, 'me ea ntlafatsa kutloisiso ea insulin, ea netefatsa li-ACC e le liphofu tsa lithethefatsi tse khahlanong le botenya le li-antidiabetes. |
| CPD1592 | ND-630 | ND-630 ke inhibitor ea acetyl-CoA carboxylase (ACC); e thibela ACC1 ea motho le ACC2 ka IC50 boleng ba 2.1 le 6.1 nM, ka ho latellana. |
