| Ologbo # | Orukọ ọja | Apejuwe |
| CPD100603 | MDK36122 | MDK36122, ti a tun mọ ni H-PGDS Inhibitor I, jẹ Prostaglandin D Synthase (hematopoietic-type) inhibitor. MDK36122 ni o ni ko koodu orukọ, ati ki o ni CAS # 1033836-12-2. Awọn ti o kẹhin 5-nọmba ti a lo fun orukọ fun rorun ibaraẹnisọrọ. MDK36122 yiyan awọn bulọọki HPGDS (IC50s = 0.7 ati 32 nM ni enzymu ati awọn igbelewọn cellular, lẹsẹsẹ) pẹlu iṣẹ ṣiṣe kekere si awọn enzymu eniyan ti o ni ibatan L-PGDS, mPGES, COX-1, COX-2, ati 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, ti a tun mọ ni ORF-20485; RWJ-20485; jẹ inhibitor 5-lipoxygenase ti o ni agbara fun itọju ikọ-fèé, osteoarthritis (OA). Tepoxalin ni iṣẹ inhibitory in vivo lodi si COX-1, COX-2, ati 5-LOX ninu awọn aja ni iwọn lilo ti a fọwọsi lọwọlọwọ. Tepoxalin ṣe alekun iṣẹ ṣiṣe ti antioxidant, pyrrolidine dithiocarbamate, ni attenuating tumor necrosis factor alpha-induced apoptosis ni awọn sẹẹli WEHI 164. |
| CPD100601 | Tenidap | Tenidap, ti a tun mọ ni CP-66248, jẹ inhibitor COX/5-LOX ati oludije oogun egboogi-iredodo ti cytokine ti o wa labẹ idagbasoke nipasẹ Pfizer bi itọju ti o ni ileri fun arthritis rheumatoid, ṣugbọn Pfizer dẹkun idagbasoke lẹhin ifọwọsi titaja ti kọ nipasẹ FDA ni ọdun 1996 nitori ẹdọ ati majele ti kidinrin, eyiti a sọ si awọn iṣelọpọ ti oogun naa pẹlu ohun elo thiophene ti o fa ibajẹ oxidative. |
| CPD100600 | PF-4191834 | PF-4191834 jẹ aramada, ti o lagbara ati yiyan ti kii-redox 5-lipoxygenase inhibitor ti o munadoko ninu iredodo ati irora. PF-4191834 ṣe afihan agbara ti o dara ni enzymu- ati awọn igbelewọn ti o da lori sẹẹli, bakannaa ni awoṣe eku ti iredodo nla. Awọn abajade idanwo Enzyme fihan pe PF-4191834 jẹ inhibitor 5-LOX ti o lagbara, pẹlu IC (50) = 229 +/- 20 nM. Pẹlupẹlu, o ṣe afihan isunmọ 300-agbo selectivity fun 5-LOX lori 12-LOX ati 15-LOX ati pe ko ṣe afihan iṣẹ-ṣiṣe si awọn enzymu cyclooxygenase. Ni afikun, PF-4191834 ṣe idiwọ 5-LOX ninu awọn sẹẹli ẹjẹ eniyan, pẹlu IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, ti a tun mọ ni L 663536, jẹ antagonist leukotriene. O le ṣe eyi nipa didi 5-lipoxygenase ti n ṣiṣẹ amuaradagba (FLAP), nitorina dena 5-lipoxygenase (5-LOX), ati pe o le ṣe iranlọwọ ni atọju atherosclerosis. MK-886 ṣe idiwọ iṣẹ-ṣiṣe cyclooxygenase-1 ati pe o dinku akopọ platelet. MK-886 nfa awọn ayipada ninu ọmọ sẹẹli ati mu apoptosis pọ si lẹhin itọju ailera photodynamic pẹlu hypericin. MK-886 mu ki o tumo negirosisi ifosiwewe-alpha-induced iyato ati apoptosis. |
| CPD100598 | L-691816 | L 691816 jẹ oludena ti o lagbara ti iṣesi 5-LO mejeeji in vitro ati ni ọpọlọpọ awọn awoṣe vivo. |
| CPD100597 | CMI-977 | CMI-977, ti a tun mọ ni LPD-977 ati MLN-977, jẹ onidalẹkun 5-lipoxygenase ti o lagbara ti o laja ni iṣelọpọ awọn leukotrienes ati pe o ti ni idagbasoke lọwọlọwọ fun itọju ikọ-fèé onibaje. CMI-977 ṣe idiwọ ọna ọna igbona 5-lipoxygenase (5-LO) cellular lati dena iran ti awọn leukotrienes, eyiti o ṣe ipa pataki ninu nfa ikọ-fèé ikọ-fèé. |
| CPD100596 | CJ-13610 | CJ-13610 jẹ inhibitor ti nṣiṣe lọwọ ẹnu ti 5-lipoxygenase (5-LO). CJ-13610 ṣe idiwọ biosynthesis ti leukotriene B4 ati ṣe ilana ikosile IL-6 mRNA ni awọn macrophages. O jẹ doko ni awọn awoṣe preclinical ti irora. |
| CPD100595 | BRP-7 | BRP-7 jẹ amuaradagba amuṣiṣẹ 5-LO (FLAP) inhibitor. |
