MPAKA # | Dzina lazogulitsa | Kufotokozera |
CPD100603 | Mtengo wa MDK36122 | MDK36122, yomwe imadziwikanso kuti H-PGDS Inhibitor I, ndi Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 ilibe code code, ndipo ili ndi CAS#1033836-12-2. Manambala 5 omaliza adagwiritsidwa ntchito kutchula dzina kuti azilumikizana mosavuta. MDK36122 imatsekereza HPGDS (IC50s = 0.7 ndi 32 nM mu ma enzyme ndi kuyesa kwa ma cell, motsatana) popanda kuchitapo kanthu motsutsana ndi ma enzymes aumunthu L-PGDS, mPGES, COX-1, COX-2, ndi 5-LOX. |
CPD100602 | Tepoxalin | Tepoxalin, yomwe imadziwikanso kuti ORF-20485; RWJ-20485; ndi 5-lipoxygenase inhibitor yomwe ingathe kuchiza mphumu, osteoarthritis (OA). Tepoxalin ali mu vivo inhibitory ntchito motsutsana ndi COX-1, COX-2, ndi 5-LOX mwa agalu pa mlingo wovomerezeka wamakono. Tepoxalin imakulitsa ntchito ya antioxidant, pyrrolidine dithiocarbamate, pochepetsa tumor necrosis factor alpha-induced apoptosis mu WEHI 164 maselo. |
CPD100601 | Tenidap | Tenidap, yemwe amadziwikanso kuti CP-66248, ndi COX/5-LOX inhibitor ndi cytokine-modulating anti-inflammatory drug candidate yomwe inali pansi pa Pfizer monga chithandizo chodalirika cha nyamakazi ya nyamakazi, koma Pfizer anaimitsa chitukuko pambuyo povomerezedwa ndi malonda. ndi FDA mu 1996 chifukwa cha kawopsedwe ka chiwindi ndi impso, zomwe zimatchedwa metabolites. mankhwala okhala ndi thiophene moiety omwe adawononga kuwonongeka kwa okosijeni. |
CPD100600 | PF-4191834 | PF-4191834 ndi buku, lamphamvu komanso losankha lomwe si redox 5-lipoxygenase inhibitor lomwe limagwira ntchito pa kutupa ndi kupweteka. PF-4191834 imawonetsa potency yabwino mu ma enzyme- ndi ma cell-based assays, komanso mumtundu wa makoswe otupa kwambiri. Zotsatira za kuyesa kwa enzyme zikuwonetsa kuti PF-4191834 ndi inhibitor yamphamvu ya 5-LOX, yokhala ndi IC(50) = 229 +/- 20 nM. Kuphatikiza apo, idawonetsa pafupifupi 300-fold selectivity ya 5-LOX pa 12-LOX ndi 15-LOX ndipo ikuwonetsa palibe ntchito yokhudzana ndi michere ya cyclooxygenase. Kuonjezera apo, PF-4191834 imalepheretsa 5-LOX m'maselo a magazi a munthu, ndi IC (80) = 370 +/- 20 nM. |
CPD100599 | Mtengo wa MK-886 | MK-886, yemwenso amadziwika kuti L 663536, ndi mdani wa leukotriene. Ikhoza kuchita izi poletsa 5-lipoxygenase activating protein (FLAP), motero imalepheretsa 5-lipoxygenase (5-LOX), ndipo ingathandize kuchiza atherosclerosis. MK-886 imalepheretsa ntchito ya cyclooxygenase-1 ndikupondereza kuphatikizika kwa mapulateleti. MK-886 imapangitsa kusintha kwa ma cell ndikuwonjezera apoptosis pambuyo pa photodynamic mankhwala ndi hypericin. MK-886 imapangitsa kusiyana kwa tumor necrosis factor-alpha-induced differentiation ndi apoptosis. |
CPD100598 | L-691816 | L 691816 ndi inhibitor yamphamvu ya 5-LO reaction in vitro komanso mitundu ingapo yama vivo. |
CPD100597 | CMI-977 | CMI-977, yomwe imadziwikanso kuti LPD-977 ndi MLN-977, ndi inhibitor yamphamvu ya 5-lipoxygenase yomwe imalowerera pakupanga ma leukotrienes ndipo pakali pano ikupangidwira kuchiza mphumu yosatha. CMI-977 imaletsa njira ya 5-lipoxygenase (5-LO) yotupa ma cell kuti itseke m'badwo wa leukotrienes, womwe umathandizira kwambiri pakuyambitsa mphumu ya bronchial. |
CPD100596 | Mtengo wa CJ-13610 | CJ-13610 ndi choletsa pakamwa cha 5-lipoxygenase (5-LO) . CJ-13610 imalepheretsa biosynthesis ya leukotriene B4 ndikuwongolera IL-6 mRNA mawu mu macrophages. Ndiwothandiza mu zitsanzo zowawa za preclinical. |
CPD100595 | BRP-7 | BRP-7 ndi 5-LO activating protein (FLAP) inhibitor. |