| CAT # | Izina ryibicuruzwa | Ibisobanuro |
| CPD100616 | Emricasan | Emricasan, uzwi kandi ku izina rya IDN 6556 na PF 03491390, ni inzitizi ya mbere mu cyiciro cya caspase inhibitor mu bigeragezo bivura indwara z’umwijima. Emricasan (IDN-6556) igabanya imvune yumwijima na fibrosis muburyo bwa murine bwa steatohepatitis idafite inzoga. IDN6556 yorohereza marginal mass islet engmentment ya porcine islet autotransplant moderi. IDN-6556 yo mu kanwa irashobora kugabanya ibikorwa bya aminotransferase kubarwayi barwaye hepatite idakira C. PF-03491390 itangwa mu kanwa igumana umwijima igihe kirekire hamwe na sisitemu nkeya, ikagira ingaruka za hepatoprotective kurwanya alfa-fas iterwa n'umwijima muburyo bw'imbeba. . |
| CPD100615 | Q-VD-Oph | QVD-OPH, izwi kandi nka Quinoline-Val-Asp-Difluorophenoxymethylketone, ni inzitizi nini ya caspase inhibitor ifite imiti igabanya ubukana. Q-VD-OPh irinda indwara ya neonatal mu mbeba ya P7: uruhare rwuburinganire. Q-VD-OPh ifite ingaruka zo kurwanya leukemia kandi irashobora gukorana na vitamine D igereranya kugirango HPK1 yerekana ibimenyetso muri selile AML. Q-VD-OPh igabanya apoptose iterwa nihungabana kandi igahindura imikorere yimikorere yinyuma yimbeba nyuma yimvune yumugongo |
| CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk ni selile-yinjira, idasubirwaho inhibitor ya caspase-3. Caspase-3 ni poroteyine yihariye ya sisitemuine igira uruhare runini muri apoptose. |
| CPD100613 | Z-IETD-FMK | MDK4982, izwi kandi nka Z-IETD-FMK, ni imbaraga zikomeye, zinjira mu ngirabuzimafatizo, zidashobora gusubira inyuma za caspase-8 na granzyme B., Caspase-8 Inhibitor II igenzura ibikorwa by’ibinyabuzima bya Caspase-8. MDK4982 ibuza neza virusi ya grippe iterwa na selile ya HeLa. MDK4982 nayo ibuza granzyme B. MDK4982 ifite CAS # 210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK ni selile-yinjira, idasubirwaho pan-caspase inhibitor. Z-VAD-FMK ibuza gutunganya caspase no kwinjiza apoptose muri selile yibibyimba muri vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, izwi kandi ku izina rya VX-765, yagenewe kubuza Caspase, iyo ikaba ari enzyme igenzura ibisekuruza bibiri bya cytokine, IL-1b na IL-18. VX-765 yerekanwe kubuza gufatwa gukabije muburyo bwa preclinical. Mubyongeyeho, VX-765 yerekanye ibikorwa muburyo bwa preclinical epilepsy idakira. VX-765 yari imaze kwipimisha ku barwayi barenga 100 mu cyiciro cya mbere cy’icyiciro cya I n’icyiciro cya IIa kijyanye n’izindi ndwara, harimo n’iminsi 28 y’amavuriro ya IIa ku barwayi barwaye psoriasis. Yasoje icyiciro cyo kuvura icyiciro cya IIa cyamavuriro ya VX-765 yandikishije abarwayi bagera kuri 75 bafite igicuri kitarwanya imiti. Ikigeragezo cya kabiri-gihumye, cyateganijwe, kigenzurwa na platbo cyateguwe hagamijwe gusuzuma umutekano, kwihanganira ibikorwa byubuvuzi bya VX-765. |
| CPD100610 | Maraviroc | Maraviroc ni antiviral, ikomeye, idahiganwa CKR-5 reseptor antagonist ibuza guhuza virusi ya virusi ya virusi gp120. Maraviroc ibuza MIP-1β-iterwa na γ-S-GTP ihuza ingirabuzimafatizo ya HEK-293, byerekana ubushobozi bwayo bwo guhagarika imiti iterwa na chemokine iterwa no guhana kwa GDP-GTP ku ruganda rwa poroteyine CKR-5 / G. Maraviroc irabuza kandi ibyabaye munsi ya chemokine iterwa na calcium yo mu bwoko bwa calcium. |
| CPD100609 | Resatorvid | Resatorvid, izwi kandi ku izina rya TAK-242, ni ingirabuzimafatizo ya selile ya TLR4 yerekana ibimenyetso, ikabuza LPS iterwa na NO, TNF-α, IL-6, na IL-1β muri macrophage ifite agaciro ka IC50 ifite agaciro ka 1-11 nM. Resatorvid ihuza guhitamo TLR4 kandi ikabangamira imikoranire hagati ya TLR4 na molekile zayo. Resatorvid itanga neuroprotection mugukomeretsa ubwonko bwubwonko: uruhare mukuvura ibikomere byubwonko bwabantu |
| CPD100608 | BAZA-Inhibitor-10 | ASK1 Inhibitor 10 ni bioavailable yo mu kanwa inhibitor ya apoptose ibimenyetso-bigenga kinase 1 (ASK1). Ihitamo kuri ASK1 hejuru ya ASK2 kimwe na MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, na B-RAF. Irabuza kwiyongera kwa streptozotocine iterwa na JNK na p38 fosifora muri selile INS-1 pancreatic β selile muburyo bushingiye kumitekerereze. |
| CPD100607 | K811 | K811 ni ASK1 yihariye inhibitor yongerera igihe cyo kubaho muburyo bwimbeba ya amyotrophique lateral sclerose. K811 yabujije neza gukwirakwiza selile mumirongo ya selile hamwe nimvugo ndende ya ASK1 no muri HER2-ikabije cyane ingirabuzimafatizo za GC. Umuti hamwe na K811 wagabanije ubunini bwibibyimba bya xenograft mugabanya ibimenyetso byikwirakwizwa. |
| CPD100606 | K812 | K812 ni inhibitor ya ASK1 yavumbuwe kugirango irambe kuramba muburyo bwimbeba ya amyotrophique lateral sclerose. |
| CPD100605 | MSC-2032964A | MSC 2032964A ninzitizi ikomeye kandi ihitamo ASK1 inhibitor (IC50 = 93 nM). Ihagarika LPS iterwa na ASK1 na p38 fosifora muri astrocytes yimbeba yimico kandi ikumira neuroinflammation muburyo bwimbeba EAE. MSC 2032964A ni munwa bioavailable kandi yinjira mubwonko. |
| CPD100604 | Selonsertib | Selonsertib, izwi kandi ku izina rya GS-4997, ni bioavailable yo mu kanwa ya inhibitor ya signal ya apoptose igenga kinase 1 (ASK1), hamwe nibikorwa bishobora kurwanya inflammatory, antineoplastique na anti-fibrotic. Intego ya GS-4997 kandi ihuza na catalitike ya kinase ya ASK1 muburyo bwa ATP irushanwa, bityo ikabuza fosifora no gukora. GS-4997 irinda umusaruro wa cytokine ikongora, igabanya-imiterere ya gen zigira uruhare muri fibrosis, ikumira apoptose ikabije kandi ikabuza ikwirakwizwa rya selile. |
| CPD100603 | MDK36122 | MDK36122, izwi kandi nka H-PGDS Inhibitor I, ni Prostaglandin D Synthase (ubwoko bwa hematopoietic). MDK36122 nta zina rya code ifite, kandi ifite CAS # 1033836-12-2. Imibare 5 yanyuma yakoreshejwe mwizina ryitumanaho ryoroshye. MDK36122 ihitamo guhitamo HPGDS (IC50s = 0.7 na 32 nM muri enzyme na selile selile) hamwe nibikorwa bike birwanya imisemburo yabantu ifitanye isano L-PGDS, mPGES, COX-1, COX-2, na 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, izwi kandi nka ORF-20485; RWJ-20485; ni 5-lipoxygenase inhibitor ishobora kuvura asima, osteoarthritis (OA). Tepoxalin ifite ibikorwa byo kubuza vivo kurwanya COX-1, COX-2, na 5-LOX mu mbwa kuri dosiye yemewe ubu. Tepoxalin yongera ibikorwa bya antioxydeant, pyrrolidine dithiocarbamate, muguhuza ibibyimba bya nekrosis yibintu alpha-iterwa na apoptose muri selile WEHI 164. |
| CPD100601 | Tenidap | Tenidap, izwi kandi ku izina rya CP-66248, ni inhibitor ya COX / 5-LOX hamwe n’umukandida w’imiti igabanya ubukana bwa cytokine-moduline yari irimo gutezwa imbere na Pfizer nk'umuti ushobora kuvura indwara ya rubagimpande, ariko Pfizer yahagaritse iterambere nyuma yo kwemererwa kwamamaza. na FDA mu 1996 kubera uburozi bwumwijima nimpyiko, byatewe na metabolite yibiyobyabwenge hamwe na thiophene moiety yangiza okiside. |
| CPD100600 | PF-4191834 | PF-4191834 nigitabo gishya, gikomeye kandi cyatoranijwe kitari redox 5-lipoxygenase inhibitor ikora neza mugutwika no kubabara. PF-4191834 yerekana imbaraga nziza muri enzyme- na selile zishingiye ku ngirabuzimafatizo, ndetse no muburyo bw'imbeba yo gutwika gukabije. Ibisubizo bya Enzyme byerekana ko PF-4191834 ari inhibitor ikomeye 5-LOX, hamwe na IC (50) = 229 +/- 20 nM. Byongeye kandi, yerekanye guhitamo inshuro zigera kuri 300 kuri 5-LOX hejuru ya 12-LOX na 15-LOX kandi ntigaragaza ibikorwa bijyanye na enzymes ya cyclooxygenase. Byongeye kandi, PF-4191834 ibuza 5-LOX mu ngirangingo z'amaraso y'abantu, hamwe na IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, izwi kandi nka L 663536, ni antagonist leukotriene. Irashobora kubikora muguhagarika 5-lipoxygenase ikora proteine (FLAP), bityo ikabuza 5-lipoxygenase (5-LOX), kandi irashobora gufasha mukuvura aterosklerose. MK-886 ibuza ibikorwa bya cyclooxygenase-1 kandi ikabuza gukusanya platine. MK-886 itera impinduka mumuzunguruko kandi ikongera apoptose nyuma yo kuvura Photodynamic hamwe na hypericine. MK-886 yongerera ikibyimba necrosis factor-alpha iterwa no gutandukana na apoptose. |
| CPD100598 | L-691816 | L 691816 ni inhibitor ikomeye ya reaction ya 5-LO haba muri vitro ndetse no muburyo bwa vivo. |
| CPD100597 | CMI-977 | CMI-977, izwi kandi nka LPD-977 na MLN-977, ni inibitori ikomeye ya lipoxygenase 5 yivanga mu musaruro wa leukotriène kandi ubu irimo gutezwa imbere mu kuvura asima idakira. CMI-977 ibuza inzira ya 5-lipoxygenase (5-LO) inzira yo gutwika ingirabuzimafatizo kugirango ibuze ibisekuruza bya leukotriène, bigira uruhare runini mu gutera asima ya bronhia. |
| CPD100596 | CJ-13610 | CJ-13610 ni inzitizi ikora mu kanwa ya 5-lipoxygenase (5-LO). CJ-13610 ibuza biosynthesis ya leukotriene B4 kandi igenga imvugo ya IL-6 mRNA muri macrophage. Nibyiza muburyo bwa preclinical ububabare. |
| CPD100595 | BRP-7 | BRP-7 ni 5-LO ikora poroteyine (FLAP) inhibitor. |
| CPD100594 | TT15 | TT15 ni agoniste wa GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 ni glucagon ya CNS-yinjira muri peptide ya peptide 1 yakira (GLP-1R) moderi nziza ya allosteric modulator (PAM) |
