IKATI # | Igama Lomkhiqizo | Incazelo |
I-CPD100603 | I-MDK36122 | I-MDK36122, eyaziwa nangokuthi i-H-PGDS Inhibitor I, iyi-Prostaglandin D Synthase (uhlobo lwe-hematopoietic) Inhibitor. I-MDK36122 ayinalo igama lekhodi, futhi ine-CAS#1033836-12-2. Amadijithi angu-5 wokugcina asetshenziselwe igama ukuze kube lula ukuxhumana. I-MDK36122 ivimba ngokukhetha i-HPGDS (IC50s = 0.7 kanye ne-32 nM kuma-enzyme nama-assay amaselula, ngokulandelana) nomsebenzi omncane ngokumelene nama-enzyme womuntu ahlobene L-PGDS, mPGES, COX-1, COX-2, kanye ne-5-LOX. |
I-CPD100602 | I-Tepoxalin | I-Tepoxalin, eyaziwa nangokuthi i-ORF-20485; I-RWJ-20485; iyi-5-lipoxygenase inhibitor engase ibe ukwelashwa kwesifuba somoya, i-osteoarthritis (OA). I-Tepoxalin inomsebenzi wokuvimbela invivo ngokumelene ne-COX-1, i-COX-2, ne-5-LOX ezinjeni kumthamo onconywayo wamanje ovunyelwe.I-Tepoxalin ivimbela ukuvuvukala kanye nokungasebenzi kahle kwe-microvascular okubangelwa i-irradiation yesisu kumagundane. I-Tepoxalin ithuthukisa umsebenzi we-antioxidant, i-pyrrolidine dithiocarbamate, ekunciphiseni i-tumor necrosis factor alpha-induced apoptosis kumaseli we-WEHI 164. |
I-CPD100601 | I-Tenidap | I-Tenidap, eyaziwa nangokuthi i-CP-66248, iyi-COX/5-LOX inhibitor kanye ne-cytokine-modulating anti-inflammatory ikhandidethi eyayisathuthukiswa yi-Pfizer njengendlela yokwelapha ethembisayo ye-rheumatoid arthritis, kodwa u-Pfizer wayimisa intuthuko ngemva kokunqatshwa kwemvume yokumaketha. yi-FDA ngo-1996 ngenxa yobuthi besibindi nezinso, okwakuthiwa kubangelwa ama-metabolites omuthi ane-thiophene moiety eyadala umonakalo we-oxidative. |
I-CPD100600 | PF-4191834 | I-PF-4191834 iyinoveli, enamandla futhi ekhethiwe engeyona i-redox 5-lipoxygenase inhibitor esebenza kahle ekuvuvukeni nasebuhlungu. I-PF-4191834 ibonisa amandla amahle kuma-enzyme- kanye nokuhlolwa okusekelwe kumaseli, kanye nemodeli yegundane yokuvuvukala okunamandla. Imiphumela yokuhlolwa kwe-enzyme ibonisa ukuthi i-PF-4191834 iyi-5-LOX inhibitor enamandla, ene-IC(50) = 229 +/- 20 nM. Ngaphezu kwalokho, ibonise ukukhethwa kwe-300-fold for 5-LOX phezu kwe-12-LOX ne-15-LOX futhi ayibonisi umsebenzi kuma-enzyme e-cyclooxygenase. Ngaphezu kwalokho, i-PF-4191834 ivimbela i-5-LOX kumaseli egazi lomuntu, nge-IC (80) = 370 +/- 20 nM. |
I-CPD100599 | I-MK-886 | I-MK-886, eyaziwa nangokuthi i-L 663536, iyimbangi ye-leukotriene. Ingenza lokhu ngokuvimbela i-5-lipoxygenase activating protein (FLAP), ngaleyo ndlela ivimbele i-5-lipoxygenase (5-LOX), futhi ingasiza ekwelapheni i-atherosclerosis. I-MK-886 ivimbela umsebenzi we-cyclooxygenase-1 futhi icindezela ukuhlanganiswa kweplatelet. I-MK-886 yenza izinguquko kumjikelezo weseli futhi ikhulise i-apoptosis ngemva kokwelashwa kwe-photodynamic nge-hypericin. I-MK-886 ithuthukisa ukuhlukaniswa kwe-tumor necrosis factor-alpha-induced and apoptosis. |
I-CPD100598 | L-691816 | I-L 691816 iyisivimbeli esinamandla sokusabela kwe-5-LO kokubili ku-vitro nakuhlu lwamamodeli e-vivo. |
I-CPD100597 | I-CMI-977 | I-CMI-977, eyaziwa nangokuthi i-LPD-977 kanye ne-MLN-977, iyi-5-lipoxygenase inhibitor enamandla engenelela ekukhiqizweni kwe-leukotrienes futhi okwamanje yenzelwe ukwelapha isifuba somoya esingamahlalakhona. I-CMI-977 ivimbela indlela yokuvuvukala kwamaselula ye-5-lipoxygenase (5-LO) ukuze ivimbele ukukhiqizwa kwe-leukotrienes, edlala indima ebalulekile ekuqaliseni i-asthma ye-bronchial. |
I-CPD100596 | I-CJ-13610 | I-CJ-13610 iyisivimbeli esisebenzayo somlomo se-5-lipoxygenase (5-LO) . I-CJ-13610 ivimbela i-biosynthesis ye-leukotriene B4 futhi ilawula inkulumo ye-IL-6 mRNA kuma-macrophages. Isebenza kahle kumamodeli angaphambi komtholampilo obuhlungu. |
I-CPD100595 | I-BRP-7 | I-BRP-7 iyi-5-LO activating protein (FLAP) inhibitor. |