| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100616 | Emricasan | I-Emricasan, eyaziwa nangokuthi i-IDN 6556 kanye ne-PF 03491390, iyi-inhibitor ye-caspase esezingeni lokuqala ekuhlolweni kwemitholampilo yokwelashwa kwezifo zesibindi. I-Emricasan (IDN-6556) inciphisa ukulimala kwesibindi kanye ne-fibrosis kumodeli ye-murine ye-non-alcohol steatohepatitis. I-IDN6556 isiza ukufakwa kweziqhingi eziseceleni kumodeli ye-porcine islet autotransplant. I-IDN-6556 yomlomo ingase yehlise umsebenzi we-aminotransferase ezigulini ezine-hepatitis C engapheli. I-PF-03491390 elawulwa ngomlomo igcinwe esibindi isikhathi eside ngokuchayeka okuphansi kwesistimu, okwenza umphumela we-hepatoprotective ngokumelene nokulimala kwesibindi kwe-alpha-fas kumodeli yegundane. . |
| I-CPD100615 | Q-VD-Oph | I-QVD-OPH, eyaziwa nangokuthi i-Quinoline-Val-Asp-Difluorophenoxymethylketone, iyi-spectrum ebanzi ye-caspase inhibitor enezici ezinamandla zokulwa ne-apoptotic. I-Q-VD-OPh ivimbela ukushaywa kwengane esanda kuzalwa ku-P7 rat: indima yobulili. I-Q-VD-OPh inemiphumela elwa ne-leukemia futhi ingasebenzisana nama-analogi ka-vitamin D ukuze kwandiswe ukusayinda kwe-HPK1 kumaseli e-AML. I-Q-VD-OPh inciphisa i-apoptosis ebangelwa ukuhlukumezeka futhi ithuthukise ukutholakala kokusebenza kwesitho sangemuva kumagundane ngemva kokulimala komgogodla. |
| I-CPD100614 | Z-DEVD-FMK | I-Z-DEVD-fmk iyi-cell-permeable, inhibitor engabuyiseleki emuva ye-caspase-3. I-Caspase-3 iyi-cysteineyl aspartate-specific protease edlala indima ebalulekile ku-apoptosis. |
| I-CPD100613 | Z-IETD-FMK | I-MDK4982, eyaziwa nangokuthi i-Z-IETD-FMK, iyisivimbeli esinamandla, esikwaziyo ukungena kuseli, esingahlehliseki emuva se-caspase-8 kanye ne-granzyme B., i-Caspase-8 Inhibitor II ilawula umsebenzi webhayoloji we-Caspase-8. I-MDK4982 ivimbela ngempumelelo i-apoptosis ebangelwa igciwane lomkhuhlane kumaseli e-HeLa. I-MDK4982 iphinde ivimbele i-granzyme B. I-MDK4982 ine-CAS#210344-98-2. |
| I-CPD100612 | Z-VAD-FMK | I-Z-VAD-FMK iyi-cell-permeable, i-pan-caspase inhibitor engabuyiseleki emuva. I-Z-VAD-FMK ivimbela ukucutshungulwa kwe-caspase kanye nokungeniswa kwe-apoptosis kumaseli wesimila ku-vitro (IC50 = 0.0015 - 5.8 mM). |
| I-CPD100611 | I-Belnacasan | I-Belnacasan, eyaziwa nangokuthi i-VX-765, yakhelwe ukuvimbela i-Caspase, okuyi-enzyme elawula ukukhiqizwa kwama-cytokines amabili, i-IL-1b ne-IL-18. I-VX-765 ikhonjiswe ukuthi ivimbela ukuquleka okunamandla kumamodeli angaphambi komtholampilo. Ngaphezu kwalokho, i-VX-765 ibonise umsebenzi kumamodeli we-preclinical wesithuthwane esingamahlalakhona. I-VX-765 yayinikwe umthamo ezigulini ezingaphezu kwe-100 ezivivinyweni zomtholampilo zesigaba-I kanye nesigaba-IIa eziphathelene nezinye izifo, kuhlanganise nokuhlolwa komtholampilo kwesigaba-IIa sezinsuku ezingama-28 ezigulini ezine-psoriasis. Iqede isigaba sokwelashwa se-phase-IIa yokuhlolwa komtholampilo kwe-VX-765 ebhalise cishe iziguli ezingama-75 ezinesithuthwane esingazweli ekwelashweni. Isilingo somtholampilo esingaboni kabili, esingahleliwe, esilawulwa yi-placebo saklanyelwe ukuhlola ukuphepha, ukubekezelelana kanye nomsebenzi womtholampilo we-VX-765. |
| I-CPD100610 | Maraviroc | I-Maraviroc iyi-antiviral, enamandla, engancintisani ne-CKR-5 receptor antagonist evimbela ukuboshwa kwe-HIV viral coat protein gp120. I-Maraviroc ivimbela i-MIP-1β-stimulated γ-S-GTP ebophezela ku-HEK-293 cell membranes, ebonisa amandla ayo okuvimbela ukukhuthazwa okuncike ku-chemokine kokushintshaniswa kwe-GDP-GTP ku-CKR-5/G protein complex. I-Maraviroc iphinde ivimbele umcimbi ongezansi wokusabalalisa kabusha kwe-calcium ye-calcium ye-chemokine-induced intracellular. |
| I-CPD100609 | I-Resatorvid | I-Resatorvid, eyaziwa nangokuthi i-TAK-242, i-cell-permeable inhibitor yokusayina kwe-TLR4, ivimbela ukukhiqizwa okwenziwe yi-LPS kwe-NO, TNF-α, IL-6, ne-IL-1β kuma-macrophages anamanani e-IC50 we-1-11 nM. I-Resatorvid ibophezela ngokukhetha ku-TLR4 futhi iphazamisa ukuxhumana phakathi kwe-TLR4 nama-athomu ayo e-adaptha. I-Resatorvid ihlinzeka nge-neuroprotection ekulimazeni okulimazayo kokuhlolwa kobuchopho: okushiwo ekwelapheni ukulimala kobuchopho bomuntu |
| I-CPD100608 | ASK1-Inhibitor-10 | I-ASK1 Inhibitor 10 iyi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1). Iyakhetha ku-ASK1 phezu kwe-ASK2 kanye ne-MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, ne-B-RAF. Ivimbela ukwanda kwe-streptozotocin-induced ku-JNK kanye ne-p38 phosphorylation kumaseli we-INS-1 we-pancreatic β ngendlela encike ekugxilweni. |
| I-CPD100607 | K811 | I-K811 iyisivimbeli esiqondene ne-ASK1 esandisa isikhathi sokusinda kumodeli yegundane ye-amyotrophic lateral sclerosis. I-K811 ivimbele ngempumelelo ukwanda kwamaseli kolayini beseli abanesisho esiphezulu esingu-ASK1 kanye namaseli e-GC e-HER2-overexpressing overexpressing. Ukwelashwa nge-K811 kuncishiswe osayizi bamathumba e-xenograft ngokwehlisa izimpawu zokusabalala. |
| I-CPD100606 | K812 | I-K812 iyisivimbeli esiqondene ne-ASK1 esitholwe ukwandisa isikhathi sokusinda kumodeli yegundane ye-amyotrophic lateral sclerosis. |
| I-CPD100605 | I-MSC-2032964A | I-MSC 2032964A iyi-ASK1 inhibitor enamandla futhi ekhethayo (IC50 = 93 nM). Ivimba i-ASK1 eyenziwe nge-LPS kanye ne-p38 phosphorylation kuma-astrocyte egundane elikhulisiwe futhi icindezela ukuvuvukala kwe-neuroinflammation kumodeli ye-EAE yegundane. I-MSC 2032964A iyatholakala nge-bioavailable ngomlomo futhi ingena ebuchosheni. |
| I-CPD100604 | I-Selonsertib | I-Selonsertib, eyaziwa nangokuthi i-GS-4997, iyi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1), enekhono lokulwa nokuvuvukala, i-antineoplastic kanye ne-anti-fibrotic. I-GS-4997 iqondisa futhi ibophezela kusizinda se-catalytic kinase se-ASK1 ngendlela yokuncintisana ye-ATP, ngaleyo ndlela ivimbele ukwenziwa kwayo kwe-phosphorylation nokwenziwa kusebenze. I-GS-4997 ivimbela ukukhiqizwa kwama-cytokines avuthayo, ilawula phansi ukubonakaliswa kwezakhi zofuzo ezihilelekile ku-fibrosis, icindezela i-apoptosis ngokweqile futhi ivimbele ukwanda kwamaselula. |
| 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 umuthi onesiqephu se-thiophene esidale 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. |
| I-CPD100594 | TT15 | I-TT15 iyi-agonist ye-GLP-1R. |
| I-CPD100593 | VU0453379 | I-VU0453379 iyi-CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric module (PAM) |
