CAT # | Igama lemveliso | Inkcazo |
CPD100603 | MDK36122 | I-MDK36122, eyaziwa ngokuba yi-H-PGDS Inhibitor I, yi-Prostaglandin D Synthase (uhlobo lwe-hematopoietic) Inhibitor. I-MDK36122 ayinalo igama lekhowudi, kwaye ine-CAS#1033836-12-2. Iidijithi ezi-5 zokugqibela zisetyenziselwe igama kunxibelelwano olulula. I-MDK36122 ivimbela ngokukhethiweyo i-HPGDS (IC50s = 0.7 kunye ne-32 nM kwi-enzyme kunye novavanyo lweselula, ngokulandelanayo) kunye nomsebenzi omncinci ngokuchasene ne-enzymes yabantu ehambelanayo L-PGDS, mPGES, COX-1, COX-2, kunye ne-5-LOX. |
CPD100602 | Tepoxalin | I-Tepoxalin, eyaziwa ngokuba yi-ORF-20485; RWJ-20485; yi-5-lipoxygenase inhibitor enokuthi ifumane unyango lwe-asthma, i-osteoarthritis (OA). I-Tepoxalin inomsebenzi we-vivo inhibitory ngokuchasene ne-COX-1, i-COX-2, kunye ne-5-LOX kwizinja kwi-dosage evunyiweyo yangoku evunyiweyo.I-Tepoxalin inqanda ukuvuvukala kunye nokungasebenzi kakuhle kwe-microvascular okubangelwa yi-irradiation yesisu kwiigundane. I-Tepoxalin iphakamisa umsebenzi we-antioxidant, i-pyrrolidine dithiocarbamate, ekunciphiseni i-tumor necrosis factor alpha-induced apoptosis kwiiseli ze-WEHI 164. |
CPD100601 | Tenidap | I-Tenidap, eyaziwa ngokuba yi-CP-66248, yi-COX/5-LOX inhibitor kunye ne-cytokine-modulating anti-inflammatory candidate eyayiphantsi kophuhliso nguPfizer njengonyango oluthembisayo lwe-rheumatoid arthritis, kodwa uPfizer wamisa uphuhliso emva kokuvunywa kwentengiso. yi-FDA ngo-1996 ngenxa yetyhefu kunye netyhefu yezintso, eyabalelwa kwi-metabolites yechiza kunye ne-thiophene moiety eyabangela umonakalo we-oxidative. |
CPD100600 | PF-4191834 | I-PF-4191834 iyiveli, inamandla kwaye ikhetha i-non-redox ye-5-lipoxygenase inhibitor esebenzayo ekudumbeni kunye neentlungu. I-PF-4191834 ibonisa amandla amahle kwi-enzyme- kunye nee-assays ezisekwe kwiseli, kunye nemodeli yegundane yokuvuvukala okukrakra. Iziphumo zovavanyo lwe-Enzyme zibonisa ukuba i-PF-4191834 yi-5-LOX inhibitor enamandla, ene-IC (50) = 229 +/- 20 nM. Ngaphezu koko, ibonise malunga ne-300-fold selectivity ye-5-LOX phezu kwe-12-LOX kunye ne-15-LOX kwaye ibonisa akukho msebenzi malunga ne-cyclooxygenase enzymes. Ukongezelela, i-PF-4191834 inqanda i-5-LOX kwiiseli zegazi lomntu, kunye ne-IC (80) = 370 +/- 20 nM. |
CPD100599 | MK-886 | I-MK-886, eyaziwa ngokuba yi-L 663536, ngumchasi we-leukotriene. Inokwenza oku ngokuthintela i-5-lipoxygenase activating protein (FLAP), ngaloo ndlela inqanda i-5-lipoxygenase (5-LOX), kwaye inokunceda ekuphatheni i-atherosclerosis. I-MK-886 inqanda umsebenzi we-cyclooxygenase-1 kwaye icinezela i-platelet aggregation. I-MK-886 yenza utshintsho kumjikelezo weseli kwaye yandisa i-apoptosis emva konyango lwe-photodynamic kunye ne-hypericin. I-MK-886 iphucula i-tumor necrosis factor-alpha-induced differentiation kunye ne-apoptosis. |
CPD100598 | L-691816 | I-L 691816 yi-inhibitor enamandla ye-5-LO yokusabela kokubili kwi-vitro kunye noluhlu lweemodeli ze-vivo. |
CPD100597 | CMI-977 | I-CMI-977, eyaziwa ngokuba yi-LPD-977 kunye ne-MLN-977, i-5-lipoxygenase inhibitor enamandla engenelela ekuveliseni i-leukotrienes kwaye ngoku iphuhliswa kunyango lwe-asthma engapheliyo. I-CMI-977 inqanda i-5-lipoxygenase (i-5-LO) indlela yokuvuvukala kwamaselula ukuvimbela ukuveliswa kwe-leukotrienes, edlala indima ebalulekileyo ekuqaliseni i-asthma ye-bronchial. |
CPD100596 | CJ-13610 | I-CJ-13610 yi-inhibitor esebenzayo yomlomo ye-5-lipoxygenase (5-LO) . I-CJ-13610 inqanda i-biosynthesis ye-leukotriene B4 kwaye ilawula ukubonakaliswa kwe-IL-6 mRNA kwi-macrophages. Iyasebenza kwiimodeli zangaphambili zentlungu. |
CPD100595 | BRP-7 | I-BRP-7 yi-5-LO activating protein (FLAP) inhibitor. |