| CAT # | Magaca Alaabta | Sharaxaada |
| CPD100616 | Emricasan | Emricasan, oo sidoo kale loo yaqaan IDN 6556 iyo PF 03491390, waa kaspase-ka-hortagga fasalka koowaad ee tijaabooyinka bukaan-socodka ee daaweynta cudurrada beerka. Emricasan (IDN-6556) waxay hoos u dhigtaa dhaawaca beerka iyo fibrosis ee qaabka murka ee steatohepatitis-ka aan khamriga ahayn. IDN6556 waxay sahlaysa ku-oolaynta gasiiradda yar ee gasiirada porcine islet model autotransplant. IDN-6556 afka laga yaabaa inay hoos u dhigto hawlaha aminotransferase ee bukaanada qaba cagaarshow C dabadheeraad ah. PF-03491390 afka laga maamulo ayaa lagu hayaa beerka muddo dheer oo leh soo-gaadhis nidaamsan oo hooseeya, taasoo saameyn ku leh hepatoprotective oo ka dhan ah dhaawaca beerka ee alfa-fas-ku keeno qaabka jiirka . |
| CPD100615 | Q-VD-Oph | QVD-OPH, oo sidoo kale loo yaqaan Quinoline-Val-Asp-Difluorophenoxymethylketone, waa spectrum caspase inhibitor ballaaran oo leh sifooyin antiapoptotic awood leh. Q-VD-OPh waxay ka hortagtaa istaroogga dhallaanka ee jiirka P7: doorka jinsiga. Q-VD-OPh waxay leedahay saameyn liddi ku ah leukemia-ga waxayna la falgeli kartaa fiitamiin D-ga analogga ah si loo kordhiyo calaamadaha HPK1 ee unugyada AML. Q-VD-OPh waxay hoos u dhigtaa apoptosis-ka dhaawaca ah waxayna wanaajisaa soo kabashada shaqada dhabarka ee jiirka ka dib dhaawaca laf dhabarta |
| CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk waa unug-meel-marin karo, horjooge aan laga noqon karin ee caspase-3. Caspase-3 waa cysteinyl aspartate-gaar ah protease kaas oo ka ciyaara doorka dhexe ee apoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, oo sidoo kale loo yaqaan Z-IETD-FMK, waa awood xoog leh, unug-wareejin, horjooge aan la bedeli karin ee kaspase-8 iyo granzyme B., Caspase-8 Inhibitor II waxay xakameysaa dhaqdhaqaaqa noolaha ee Caspase-8. MDK4982 waxay si wax ku ool ah u joojisaa fayraska hargabka apoptosis ee unugyada HeLa. MDK4982 sidoo kale waxay joojisaa granzyme B. MDK4982 waxay leedahay CAS # 210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK waa unug-meel-marin karo, xannibaadaha pan-caspase aan laga noqon karin. Z-VAD-FMK waxay joojisaa habaynta kasbaska iyo soo-saarka apoptosis ee unugyada burooyinka ee vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, oo sidoo kale loo yaqaan VX-765, waxaa loogu talagalay in lagu xakameeyo Caspase, taas oo ah enzyme xakameynaya jiilka laba cytokines, IL-1b iyo IL-18. VX-765 ayaa la tusay inay joojiso suuxdinta degdega ah ee moodooyinka hore. Intaa waxaa dheer, VX-765 waxay muujisay firfircoonida moodooyinka hore ee suuxdinta dabadheeraad ah. VX-765 ayaa lagu qiyaasey in ka badan 100 bukaan oo ku jira marxaladda-I iyo marxaladda-IIa tijaabooyinka bukaan-socodka ee la xiriira cudurrada kale, oo ay ku jiraan 28-maalmood-IIa tijaabo caafimaad ee bukaannada qaba cudurka psoriasis. Waxay dhammaysay wejigii daawaynta ee wajiga-IIa tijaabada caafimaad ee VX-765 taas oo diiwaangelisay ku dhawaad 75 bukaan oo qaba suuxdin u adkaysta. Laba-indho-indho la'aan, randomized, tijaabada bukaan-socod-koontarool ee placebo waxaa loogu talagalay in lagu qiimeeyo badbaadada, dulqaadka iyo dhaqdhaqaaqa bukaan-socodka ee VX-765. |
| CPD100610 | Maraviroc | Maraviroc waa ka-hortagga fayraska, awood leh, aan tartan lahayn CKR-5 antagonist receptor antagonist kaas oo xannibaya xidhitaanka borotiinka jaakad fayraska HIV gp120. Maraviroc wuxuu joojiyaa MIP-1β-kicinta γ-S-GTP ee ku xiran xuubka unugyada HEK-293, taas oo muujinaysa awoodda ay u leedahay in ay joojiso kicinta ku-tiirsanaanta chemokine ee GDP-GTP ee isweydaarsiga borotiinka CKR-5 / G. Maraviroc waxa kale oo uu hor istaagaa dhacdada hoose ee kaalshiyamka intracellular intracellular ay keentay kiimiko. |
| CPD100609 | Resatorvid | Resatorvid, oo sidoo kale loo yaqaan TAK-242, waa unug-soo-baxa xannibaadaha TLR4, xannibaya wax soo saarka LPS ee NO, TNF-α, IL-6, iyo IL-1β ee macrophages leh IC50 qiimaha 1-11 nM. Resatorvid waxay si xushmad leh ugu xidhaa TLR4 waxayna faragelisaa isdhexgalka TLR4 iyo unugyadeeda adaabta. Resatorvid waxay bixisaa neuroprotection ee dhaawaca maskaxda ee tijaabada ah: saameyn ku yeelashada daaweynta dhaawaca maskaxda bini'aadamka |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 waa horjoogaha afka laga heli karo ee apoptosis signal-regulating kinase 1 (ASK1). Waxay u dooratay ASK1 oo ka sarreeya ASK2 iyo sidoo kale MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, iyo B-RAF. Waxay joojisaa kororka streptozotocin-ku-kordhinta JNK iyo fosforyaalka p38 ee unugyada β-pancreatic ee INS-1 qaab-ku-tiirsanaan. |
| CPD100607 | K811 | K811 waa ASK1-gaar-horjooge u-dheereeya badbaadada moodeelka jiirka ee amyotrophic lateral sclerosis. K811 waxay si hufan uga hortagtay kororka unugyada ee xariiqyada gacanta ee leh muujinta sare ee ASK1 iyo HER2-unugyada GC-ga oo xad dhaaf ah. Daawaynta K811 waxay hoos u dhigtay xajmiyada burooyinka xenograft iyadoo hoos loo dhigayo calaamadaha fidinta. |
| CPD100606 | K812 | K812 waa ASK1-horjooge u gaar ah oo la helay si uu u sii dheereeyo badbaadada moodeelka jiirka ee amyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | MSC 2032964A waa mid awood leh oo la xushay ASK1 inhibitor (IC50 = 93 nM). Waxay xannibaysaa LPS-sababtoo ah ASK1 iyo fosforyaalka p38 ee jiirka dhaqameed ee astrocytes waxayna xakameysaa xanuunka neerfaha ee moodalka EAE. MSC 2032964A waa mid afka laga heli karo oo maskaxda gasha. |
| CPD100604 | Selonsertib | Selonsertib, oo sidoo kale loo yaqaan GS-4997, waa xannibaadaha afka ee apoptosis signal-regulating kinase 1 (ASK1), oo leh waxqabadyo ka-hortagga bararka, antineoplastic iyo ka-hortagga fibrotic-ka. GS-4997 waxay beegsataa oo ay ku xidhaa domainka catalytic kinase ee ASK1 si tartan ah oo ATP ah, si ay uga hortagto fosforyaalkeeda iyo hawlgelinteeda. GS-4997 waxay ka hortagtaa soo saarista cytokines bararka, waxay hoos u dhigtaa muujinta gen ee ku lug leh fibrosis, waxay xakameysaa apoptosis xad-dhaaf ah waxayna joojisaa kororka unugyada. |
| CPD100603 | MDK36122 | MDK36122, oo sidoo kale loo yaqaano H-PGDS Inhibitor I, waa Prostaglandin D Synthase (nooca hematopoietic) Inhibitor. MDK36122 ma laha magac kood, oo wuxuu leeyahay CAS#1033836-12-2. 5-ta nambar ee ugu dambeeyay waxaa loo adeegsaday magac si ay u sahlanaato isgaarsiinta. MDK36122 waxay si xushmad leh u xannibaysaa HPGDS (IC50s = 0.7 iyo 32 nM ee enzymes iyo imtixaannada gacanta, siday u kala horreeyaan) oo leh waxqabad yar oo ka dhan ah enzymes-ka aadanaha ee la xidhiidha L-PGDS, mPGES, COX-1, COX-2, iyo 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, oo sidoo kale loo yaqaan ORF-20485; RWJ-20485; waa 5-lipoxygenase inhibitor oo awood u leh daaweynta neefta, osteoarthritis (OA). Tepoxalin waxay leedahay in vivo firfircoonida inhibitory ka soo horjeeda COX-1, COX-2, iyo 5-LOX ee eeyaha ee hadda la ansixiyay qiyaasta lagu taliyey. Tepoxalin waxay wanaajisaa waxqabadka antioxidant, pyrrolidine dithiocarbamate, oo hoos u dhigaysa buro necrosis factor alfa-induced apoptosis ee unugyada WEHI 164. |
| CPD100601 | Tenidap | Tenidap, oo sidoo kale loo yaqaan CP-66248, waa COX/5-LOX inhibitor iyo cytokine-modulating anti-inflammatory drug musharax kaas oo ay ku jirtay horumarinta Pfizer si ay u noqoto daaweyn suurtagal ah oo loogu talagalay rheumatoid arthritis-ka, laakiin Pfizer ayaa joojisay horumarinta ka dib markii ogolaanshaha suuqgeynta la diiday. by FDA ee 1996 sababtoo ah sunta beerka iyo kelyaha, taas oo loo aaneeyay dheef-shiid kiimikaad ee daawada leh thiophene unug sababay waxyeello oksaydh ah. |
| CPD100600 | PF-4191834 | PF-4191834 waa sheeko cusub, awood leh oo la xushay 5-lipoxygenase inhibitor aan dib-u-habayn oo waxtar u leh bararka iyo xanuunka. PF-4191834 waxay soo bandhigaysaa awood wanaagsan oo ku jirta enzyme-iyo imtixaannada unugyada ku salaysan, iyo sidoo kale qaabka jiirka ee caabuqa ba'an. Natiijooyinka baaritaanka Enzyme waxay muujinayaan in PF-4191834 ay tahay 5-LOX inhibitor oo awood leh, oo leh IC (50) = 229 +/- 20 nM. Intaa waxaa dheer, waxay muujisay qiyaastii 300-laab xulashada 5-LOX ee 12-LOX iyo 15-LOX mana muujinayso wax dhaqdhaqaaq ah oo ku wajahan enzymes cyclooxygenase. Intaa waxaa dheer, PF-4191834 waxay joojisaa 5-LOX ee unugyada dhiigga ee bini'aadamka, oo leh IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, oo sidoo kale loo yaqaan L 663536, waa antagonist leukotriene. Waxaa laga yaabaa inay tan sameyso iyadoo xannibaysa 5-lipoxygenase activating protein (FLAP), sidaas darteed waxay joojinaysaa 5-lipoxygenase (5-LOX), waxayna kaa caawin kartaa daaweynta atherosclerosis. MK-886 wuxuu joojiyaa dhaqdhaqaaqa cyclooxygenase-1 wuxuuna xakameeyaa isku-darka platelet. MK-886 waxay keentaa isbeddel ku yimaada wareegga unugyada waxayna kordhisaa apoptosis ka dib daawaynta sawir-qaadista ee hypericin. MK-886 waxay wanaajisaa burada necrosis factor-alpha-induced farqiga iyo apoptosis. |
| CPD100598 | L-691816 | L 691816 waa horjooge awood leh falcelinta 5-LO labadaba gudaha vitro iyo noocyada kala duwan ee vivo. |
| CPD100597 | CMI-977 | CMI-977, oo sidoo kale loo yaqaan LPD-977 iyo MLN-977, waa 5-lipoxygenase inhibitor oo awood leh oo farageliya soo saarista leukotrienes waxaana hadda loo soo saaray daaweynta neefta dabadheeraad ah. CMI-977 waxay joojisaa 5-lipoxygenase (5-LO) dariiqa caabuqa unugyada si ay u xannibto jiilka leukotrienes, kaas oo door muhiim ah ka ciyaara kicinta neefta bronki. |
| CPD100596 | CJ-13610 | CJ-13610 waa ka hortag afka ah oo firfircoon ee 5-lipoxygenase (5-LO). CJ-13610 waxay joojisaa biosynthesis ee leukotriene B4 waxayna xakameysaa muujinta IL-6 mRNA ee macrophages. Waxay wax ku ool u tahay moodooyinka hore ee xanuunka. |
| CPD100595 | BRP-7 | BRP-7 waa borotiinka firfircoonida 5-LO (FLAP). |
| CPD100594 | TT15 | TT15 waa agonist ee GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 waa CNS-guulaysata glucagon-sida peptide 1 reseptor (GLP-1R) modulator togan (PAM) |
