PUSI # | Igoa Oloa | Fa'amatalaga |
CPD100603 | MDK36122 | MDK36122, faʻapitoa foi o le H-PGDS Inhibitor I, o le Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 e leai se igoa fa'ailoga, ma e iai le CAS#1033836-12-2. O le numera 5 mulimuli na faʻaaogaina mo igoa mo fesoʻotaʻiga faigofie. MDK36122 filifili poloka HPGDS (IC50s = 0.7 ma 32 nM i enzyme ma cellular assays, faasologa) faʻatasi ai ma sina gaioiga e faʻatatau i enzymes tagata L-PGDS, mPGES, COX-1, COX-2, ma le 5-LOX. |
CPD100602 | Tepoxalin | Tepoxalin, e lauiloa foi o le ORF-20485; RWJ-20485; ose 5-lipoxygenase inhibitor e mafai ona togafitia ai le sela, osteoarthritis (OA). Tepoxalin ei ai in vivo inhibitory gaoioiga e faasaga i COX-1, COX-2, ma le 5-LOX i maile i le taimi nei ua faamaonia fualaau fautuaina. Tepoxalin inhibits fula ma microvascular dysfunction faʻaosoina irradiation manava i isumu. Tepoxalin e faʻaleleia le gaioiga o se antioxidant, pyrrolidine dithiocarbamate, i le faʻaitiitia o le tumo necrosis factor alpha-induced apoptosis i WEHI 164 sela. |
CPD100601 | Tenidap | Tenidap, lea e lauiloa foi o le CP-66248, o se COX/5-LOX inhibitor ma cytokine-modulating anti-inflammatory drug candidate lea sa i lalo o le atinaeina e le Pfizer e avea o se fuafuaga manuia togafitiga mo le gugu o le rheumatoid, ae na taofia e Pfizer le atinae ina ua teena le faamaoniga maketi. e le FDA i le 1996 ona o le ate ma fatugaʻo oona, lea na mafua mai i metabolites o le vailaʻau faʻatasi ma se vaega thiophene. na mafua ai le faaleagaina o le oxidative. |
CPD100600 | PF-4191834 | PF-4191834 o se tala, malosi ma le filifilia e le redox 5-lipoxygenase inhibitor aoga i le mumū ma le tiga. O le PF-4191834 o loʻo faʻaalia ai le malosi lelei i suʻesuʻega faʻavae enzyme-ma sela, faʻapea foʻi ma se faʻataʻitaʻiga o le iole o le mumū ogaoga. Ole su'esu'ega ole enzyme e fa'aalia ai o le PF-4191834 ole malosi ole 5-LOX, ma le IC(50) = 229 +/- 20 nM. E le gata i lea, na faʻaalia pe tusa ma le 300-filifili filifiliga mo le 5-LOX i luga ole 12-LOX ma le 15-LOX ma faʻaalia e leai se gaioiga agai i le cyclooxygenase enzymes. E le gata i lea, o le PF-4191834 e taofia ai le 5-LOX i sela toto o le tagata, ma le IC(80) = 370 +/- 20 nM. |
CPD100599 | MK-886 | MK-886, e taʻua foi o le L 663536, o le leukotriene antagonist. E mafai ona faia lenei mea e ala i le polokaina o le 5-lipoxygenase activating protein (FLAP), ma taofia ai le 5-lipoxygenase (5-LOX), ma e mafai ona fesoasoani i le togafitia o le atherosclerosis. O le MK-886 e taofia ai le gaioiga o le cyclooxygenase-1 ma taofia le faʻapipiʻiina o platelet. MK-886 faʻaosofia suiga i le taamilosaga o le cell ma faʻateleina apoptosis pe a maeʻa togafitiga photodynamic ma hypericin. MK-886 faʻaleleia le tumo necrosis factor-alpha-induced differentiation ma apoptosis. |
CPD100598 | L-691816 | L 691816 ose fa'atosina malosi o le tali 5-LO e lua ile in vitro ma le tele o fa'ata'ita'iga in vivo. |
CPD100597 | CMI-977 | CMI-977, ua lauiloa foi o le LPD-977 ma le MLN-977, o se inhibitor malosi 5-lipoxygenase e faʻalavelave i le gaosiga o leukotrienes ma o loʻo atiaʻe nei mo togafitiga o le fomaʻi masani. O le CMI-977 e taofia ai le 5-lipoxygenase (5-LO) cellular inflammation auala e poloka ai le gaosiga o leukotrienes, lea e faia se sao taua i le faʻaosoina o le sela bronchial. |
CPD100596 | CJ-13610 | O le CJ-13610 o se fa'agata fa'amalosi tautala o le 5-lipoxygenase (5-LO) . CJ-13610 taofia le biosynthesis o leukotriene B4 ma faʻatonutonu le faʻamatalaga IL-6 mRNA i macrophages. E aoga i faʻataʻitaʻiga preclinical o tiga. |
CPD100595 | BRP-7 | BRP-7 o le 5-LO activating protein (FLAP) inhibitor. |