KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
CPD100603 | MDK36122 | MDK36122, e tsejoang hape e le H-PGDS Inhibitor I, ke Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 ha e na lebitso la khoutu, mme e na le CAS#1033836-12-2. Linomoro tse 5 tsa ho qetela li sebelisitsoe bakeng sa lebitso bakeng sa puisano e bonolo. MDK36122 e thibela ka mokhoa o ikhethileng HPGDS (IC50s = 0.7 le 32 nM ka li-enzyme le liteko tsa cellular, ka ho latellana) ka ts'ebetso e nyane khahlano le li-enzyme tse amanang le batho L-PGDS, mPGES, COX-1, COX-2, le 5-LOX. |
CPD100602 | Tepoxalin | Tepoxalin, e tsejoang hape e le ORF-20485; RWJ-20485; ke 5-lipoxygenase inhibitor e khonang ho phekola asthma, osteoarthritis (OA). Tepoxalin e na le ts'ebetso ea inhibitory ea vivo khahlanong le COX-1, COX-2, le 5-LOX ho lintja ka tekanyo e khothalletsoang ea hona joale e amohelehang.Tepoxalin e thibela ho ruruha le ho se sebetse ha microvascular ho bakoang ke mahlaseli a mpeng ho likhoto. Tepoxalin e ntlafatsa ts'ebetso ea antioxidant, pyrrolidine dithiocarbamate, ho attenuating tumor necrosis factor alpha-induced apoptosis liseleng tsa WEHI 164. |
CPD100601 | Tenidap | Tenidap, eo hape e tsejoang e le CP-66248, ke COX/5-LOX inhibitor le cytokine-modulating anti-inflammatory inhibitor e neng e ntse e ntlafatsoa ke Pfizer e le pheko e ts'episang bakeng sa ramatiki ea ramatiki, empa Pfizer o ile a emisa nts'etsopele kamora hore tumello ea papatso e haneloe. ke FDA ka 1996 ka lebaka la chefo ea sebete le liphio, e neng e bakoa ke metabolites ea moriana o nang le karolo ea thiophene e bakileng tšenyo ea oxidative. |
CPD100600 | PF-4191834 | PF-4191834 ke buka, e matla le e khethollang e seng redox 5-lipoxygenase inhibitor e sebetsang ho ruruha le bohloko. PF-4191834 e bonts'a potency e ntle litekong tsa enzyme- le liseleng, hammoho le mohlala oa likhoto oa ho ruruha ho matla. Liphetho tsa tlhahlobo ea enzyme li bontša hore PF-4191834 ke 5-LOX inhibitor e matla, e nang le IC(50) = 229 +/- 20 nM. Ho feta moo, e bontšitse hoo e batlang e le 300-fold selectivity bakeng sa 5-LOX holim'a 12-LOX le 15-LOX 'me e bontša ha ho mosebetsi o lebisang ho li-enzyme tsa cyclooxygenase. Ho phaella moo, PF-4191834 e thibela 5-LOX liseleng tsa mali tsa motho, tse nang le IC (80) = 370 +/- 20 nM. |
CPD100599 | MK-886 | MK-886, eo hape e tsejoang e le L 663536, ke mohanyetsi oa leukotriene. E ka etsa sena ka ho thibela 5-lipoxygenase activating protein (FLAP), kahoo e thibela 5-lipoxygenase (5-LOX), 'me e ka thusa ho phekola atherosclerosis. MK-886 e thibela ts'ebetso ea cyclooxygenase-1 mme e hatella platelet aggregation. MK-886 e etsa hore ho be le liphetoho ka potoloho ea lisele 'me e eketsa apoptosis ka mor'a phekolo ea photodynamic e nang le hypericin. MK-886 e ntlafatsa phapang ea tumor necrosis factor-alpha-induced le apoptosis. |
CPD100598 | L-691816 | L 691816 ke inhibitor e matla ea 5-LO reaction ka bobeli in vitro le mefuta e mengata ea in vivo. |
CPD100597 | CMI-977 | CMI-977, eo hape e tsejoang e le LPD-977 le MLN-977, ke inhibitor e matla ea 5-lipoxygenase e kenellang tlhahisong ea li-leukotrienes 'me e ntse e ntlafatsoa bakeng sa phekolo ea asthma e sa foleng. CMI-977 e thibela 5-lipoxygenase (5-LO) tsela ea ho ruruha ea cellular ho thibela moloko oa leukotrienes, o phethang karolo ea bohlokoa ho bakang asthma ea bronchial. |
CPD100596 | CJ-13610 | CJ-13610 ke inhibitor e sebetsang ka molomo ea 5-lipoxygenase (5-LO) . CJ-13610 e thibela biosynthesis ea leukotriene B4 mme e laola polelo ea IL-6 mRNA ho macrophages. E sebetsa hantle mefuteng ea pele ea bohloko. |
CPD100595 | BRP-7 | BRP-7 ke 5-LO activating protein (FLAP) inhibitor. |