CAT # | Inoa Huahana | wehewehe |
CPD100573 | PF-05175157 | ʻO ka PF-05175157 he mea hoʻopaneʻe ikaika a koho ʻia o ka acetyl-CoA carboxylase isoform ACC1 i loaʻa i ka ate a me ka adipose tissue a me ka isoform ACC2 mana i loko o ka iwi iwi a me ka puʻuwai puʻuwai, me nā waiwai IC50 o 27 nM a me 33 nM, kēlā me kēia. Kāohi nā mea hoʻolale ACC i ka lipogenesis de novo a hoʻonui i ka β-oxidation o nā ʻakika momona lōʻihi me ka hiki ke mālama i ka maʻi diabetes type 2, hepatic steatosis, a me ka maʻi kanesa. |
CPD100572 | ND-646 | ʻO ND-646-he mea hoʻopaneʻe allosteric o nā enzymes ACC ACC1 a me ACC2 e pale ana i ka dimerization subunit ACC-e hoʻopau i ka synthesis acid fatty in vitro a i vivo. ʻO ka mālama maʻi ND-646 o ka xenograft a me nā hiʻohiʻona ʻiole genetically engineered o NSCLC i kāohi i ka ulu ʻana o ka maʻi. Ke lawelawe ʻia ma ke ʻano he mea hoʻokahi a i hui pū ʻia me ka carboplatin lāʻau lapaʻau maʻamau, ʻo ND-646 i hoʻopaʻa nui i ka ulu ʻana o ka maʻi maʻi maʻi ma Kras; Trp53-/- (ʻike ʻia ʻo KRAS p53) a me Kras; Stk11-/- ( ʻike ʻia ʻo KRAS Lkb1) nā hiʻohiʻona ʻiole o NSCLC. Ua hoʻonui ka ND-646 i ka maikaʻi ke hui pū me ka carboplatin, kahi mea maʻamau o nā regimen chemotherapeutic i hoʻohana ʻia e mālama i ka NSCLC kanaka. |
CPD100571 | CP-640186 | ʻO CP-640186 kahi mea hoʻopale ikaika o nā ACC mammalian a hiki ke hoʻemi i ke kaumaha o ke kino a hoʻomaikaʻi i ka ʻike insulin i nā holoholona hoʻāʻo. Ua hōʻike ʻia ʻo CP-640186 i kēia manawa he mea hoʻokae ikaika o nā isoforms o nā ACC mammalian me nā waiwai IC50 ma kahi o 55 nM. ʻO kēia wale nō ka mea i hōʻike ʻia i ka mea hoʻomake nui o ka mammalian ACCs. I loko o nā moʻomeheu cell a me nā ʻano holoholona, hiki i ka CP-640186 ke hoʻemi i nā pae malonyl-CoA, kaohi ʻana i ka biosynthesis momona momona, a hoʻoulu i ka oxidation momona. ʻO ka mea nui loa, hiki i ka CP-640186 ke hōʻemi i ka nui o ka momona o ke kino a me ke kaumaha o ke kino, a hoʻomaikaʻi i ka ʻike insulin, e hōʻoia ana i nā ACC i mau pahuhopu no nā lāʻau antiobesity a me antidiabetes. |
CPD1592 | ND-630 | ʻO ND-630 kahi mea hoʻopale acetyl-CoA carboxylase (ACC); kaohi kanaka ACC1 a me ACC2 me IC50 waiwai o 2.1 a me 6.1 nM, pakahi. |