MPAKA # | Dzina lazogulitsa | Kufotokozera |
CPD100573 | PF-05175157 | PF-05175157 ndi choletsa champhamvu komanso chosankha cha acetyl-CoA carboxylase isoform ACC1 yomwe ili makamaka m'chiwindi ndi minofu ya adipose ndi isoform ACC2 yomwe imayang'anira chigoba ndi minofu yamtima, yokhala ndi IC50 milingo ya 27 nM ndi 33 nM, motsatana. ACC inhibitors inhibitor de novo lipogenesis ndikuwonjezera β-oxidation yamafuta amchere amtali omwe amatha kuchiza matenda amtundu wa 2, hepatic steatosis, ndi khansa. |
CPD100572 | Nd-646 | ND-646 ndi-allosteric inhibitor ya ACC enzymes ACC1 ndi ACC2 yomwe imalepheretsa ACC subunit dimerization-kupondereza kaphatikizidwe ka mafuta acid mu vitro ndi mu vivo. Chithandizo chamankhwala cha ND-646 cha xenograft ndi ma mbewa opangidwa ndi ma genetic a NSCLC adaletsa kukula kwa chotupa. Ikagwiritsidwa ntchito ngati wothandizira m'modzi kapena kuphatikiza ndi carboplatin yokhazikika, ND-646 imalepheretsa kukula kwa chotupa cha m'mapapo ku Kras; Trp53-/- (yomwe imadziwikanso kuti KRAS p53) ndi Kras; Stk11-/- ( amadziwikanso kuti KRAS Lkb1) mitundu ya mbewa ya NSCLC. ND-646 inali yothandiza kwambiri ikaphatikizidwa ndi carboplatin, gawo lodziwika bwino lamankhwala a chemotherapeutic omwe amagwiritsidwa ntchito pochiza NSCLC yamunthu. |
CPD100571 | Mtengo wa CP-640186 | CP-640186 ndi inhibitor yamphamvu ya mammalian ACCs ndipo imatha kuchepetsa kulemera kwa thupi ndikuwonjezera chidwi cha insulin mu nyama zoyesa. CP-640186 posachedwapa yasonyezedwa kuti ndi inhibitor yamphamvu ya isoforms ya mammalian ACCs ndi IC50 values pafupifupi 55 nM. Ichi ndiye chokhacho choletsa champhamvu cha mammalian ACC. M'maselo amtundu komanso mu zinyama, CP-640186 ikhoza kuchepetsa minofu ya malonyl-CoA, kulepheretsa mafuta a asidi biosynthesis, ndi kulimbikitsa mafuta a asidi oxidation. Chofunika kwambiri, CP-640186 ikhoza kuchepetsa mafuta a thupi ndi kulemera kwa thupi, ndikuwongolera kukhudzidwa kwa insulini, kutsimikizira ma ACC monga zolinga za antiobesity ndi antidiabetes mankhwala. |
Mtengo wa CPD1592 | Mtengo wa ND-630 | ND-630 ndi acetyl-CoA carboxylase (ACC) inhibitor; imalepheretsa ACC1 yaumunthu ndi ACC2 yokhala ndi IC50 ma values a 2.1 ndi 6.1 nM, motsatana. |