| CAT # | Igama lemveliso | Inkcazo |
| CPD100616 | Emricasan | I-Emricasan, eyaziwa ngokuba yi-IDN 6556 kunye ne-PF 03491390, yiklasi yokuqala ye-caspase inhibitor kwiimvavanyo zekliniki zonyango lwezifo zesibindi. I-Emricasan (IDN-6556) inciphisa ukulimala kwesibindi kunye ne-fibrosis kwimodeli ye-murine ye-steatohepatitis engeyiyo utywala. I-IDN6556 iququzelela ukumiliselwa kwesiqithi esiselunxwemeni kwimodeli ye-porcine islet autotransplant. I-IDN-6556 yomlomo inokunciphisa umsebenzi we-aminotransferase kwizigulane ezine-hepatitis C engapheliyo. I-PF-03491390 elawulwa ngomlomo igcinwe kwisibindi ixesha elide kunye ne-systemic exposure ephantsi, eqhuba i-hepatoprotective effect kwi-alpha-fas-induced isibindi yokulimala kwimodeli yegundane. . |
| CPD100615 | Q-VD-Oph | I-QVD-OPH, eyaziwa ngokuba yi-Quinoline-Val-Asp-Difluorophenoxymethylketone, i-wide spectrum caspase inhibitor eneempawu ezinamandla ze-antiapoptotic. I-Q-VD-OPh ikhusela i-neonatal stroke kwi-P7 rat: indima yesini. I-Q-VD-OPh ineempembelelo ezichasene ne-leukemia kwaye inokusebenzisana ne-vitamin D analogs ukunyusa ukubonakaliswa kwe-HPK1 kwiiseli ze-AML. I-Q-VD-OPh inciphisa i-apoptosis eyenziwa yi-trauma kwaye iphucula ukubuyiswa komsebenzi we-back-hend kumagundane emva kokulimala kwentambo yomgogodla. |
| CPD100614 | Z-DEVD-FMK | I-Z-DEVD-fmk yi-cell-permeable, inhibitor engenakunqandwa ye-caspase-3. I-Caspase-3 yi-cysteineyl aspartate-specific protease edlala indima ephambili kwi-apoptosis. |
| CPD100613 | Z-IETD-FMK | I-MDK4982, eyaziwa ngokuba yi-Z-IETD-FMK, inamandla, i-cell-permeable, inhibitor engenakunqandwa ye-caspase-8 kunye ne-granzyme B., I-Caspase-8 Inhibitor II ilawula umsebenzi we-biological we-Caspase-8. I-MDK4982 inqanda ngokufanelekileyo i-apoptosis eyenziwa yintsholongwane yomkhuhlane kwiiseli ze-HeLa. I-MDK4982 iphinda inqanda i-granzyme B. MDK4982 ine-CAS # 210344-98-2. |
| CPD100612 | Z-VAD-FMK | I-Z-VAD-FMK yi-cell-permeable, i-pan-caspase inhibitor engenakuguqulwa. I-Z-VAD-FMK inqanda ukusetyenzwa kwe-caspase kunye nokungeniswa kwe-apoptosis kwiiseli ze-tumor in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | I-Belnacasan, eyaziwa ngokuba yi-VX-765, yenzelwe ukuvimbela i-Caspase, eyi-enzyme elawula ukuveliswa kwee-cytokines ezimbini, i-IL-1b kunye ne-IL-18. I-VX-765 ibonakaliswe ukuba inqanda ukubanjwa okukrakra kwiimodeli zangaphambili. Ukongeza, i-VX-765 ibonise umsebenzi kwiimodeli ze-preclinical zesithuthwane esingapheliyo. I-VX-765 iye yajoliswa kwizigulane ezingaphezu kwe-100 kwi-phase-I kunye ne-phase-IIa yolingo lweklinikhi olunxulumene nezinye izifo, kubandakanywa ulingo lwezonyango lwe-28-day-IIa kwizigulane ezine-psoriasis. Igqibe isigaba sonyango lwesigaba-IIa solingo lwezonyango lwe-VX-765 olubhalise malunga nezigulane ezingama-75 ezinesithuthwane esinganyangekiyo kunyango. Ulingo lwekliniki oluyimfama oluphindwe kabini, olungahleliwe, olulawulwa yi-placebo lwenzelwe ukuvavanya ukhuseleko, ukunyamezela kunye nomsebenzi weklinikhi we-VX-765. |
| CPD100610 | Maraviroc | I-Maraviroc i-antiviral, inamandla, i-CKR-5 receptor antagonist engakhuphisaniyo ethintela ukubopha i-HIV viral coat protein gp120. I-Maraviroc inqanda i-MIP-1β-ivuselelwe i-γ-S-GTP ebophelelayo kwi-HEK-293 i-membrane yeseli, ebonisa ukukwazi kwayo ukuvimbela ukuxhomekeka kwe-chemokine-exhomekeke kwi-GDP-GTP yotshintshiselwano kwi-CKR-5 / G yeprotheyini eyinkimbinkimbi. I-Maraviroc iphinda ivimbele isiganeko esisezantsi se-chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Resatorvid | I-Resatorvid, eyaziwa nangokuthi i-TAK-242, i-cell-permeable inhibitor ye-TLR4 yokubonisa, ukuvimbela ukuveliswa kwe-LPS-induced production of NO, TNF-α, IL-6, kunye ne-IL-1β kwi-macrophages kunye ne-IC50 ixabiso le-1-11 nM. I-Resatorvid ibophelela ngokukhethekileyo kwi-TLR4 kwaye iphazamisane nokusebenzisana phakathi kwe-TLR4 kunye ne-adaptha ye-adaptha. I-Resatorvid ibonelela nge-neuroprotection kuvavanyo lokwenzakala kwengqondo: impembelelo kunyango lokwenzakala kwengqondo yomntu |
| CPD100608 | ASK1-Inhibitor-10 | I-ASK1 Inhibitor 10 yi-oral bioavailable inhibitor ye-apoptosis signal-regulating kinase 1 (ASK1). Ikhetha i-ASK1 phezu kwe-ASK2 kunye ne-MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, kunye ne-B-RAF. Ivimbela ukunyuka okubangelwa yi-streptozotocin kwi-JNK kunye ne-p38 phosphorylation kwi-INS-1 i-pancreatic β cells ngendlela exhomekeke kuyo. |
| CPD100607 | K811 | I-K811 yi-ASK1-specific inhibitor eyenza ixesha elide ukusinda kwimodeli ye-mouse ye-amyotrophic lateral sclerosis. I-K811 ikhusele ngokufanelekileyo ukwanda kweeseli kwimizila yeeseli kunye nenkcazo ephezulu ye-ASK1 kunye nakwiiseli ze-GC ze-HER2-overexpressing. Unyango nge-K811 lucuthe ubungakanani bamathumba e-xenograft ngokunciphisa iimpawu zokwanda. |
| CPD100606 | K812 | I-K812 yi-ASK1-specific inhibitor efunyenwe ukwandisa ukusinda kwimodeli ye-mouse ye-amyotrophic lateral sclerosis. |
| CPD100605 | I-MSC-2032964A | I-MSC 2032964A inamandla kwaye i-ASK1 inhibitor ekhethiweyo (IC50 = 93 nM). Ivimba i-ASK1 eyenziwe yi-LPS kunye ne-p38 phosphorylation kwi-astrocyte yemouse ekhuliswe kwaye icinezela i-neuroinflammation kwimodeli ye-EAE ye mouse. I-MSC 2032964A ifumaneka ngomlomo kwaye ingena ebuchotsheni. |
| CPD100604 | Selonsertib | I-Selonsertib, eyaziwa ngokuba yi-GS-4997, yi-inhibitor ye-bioavailable yomlomo ye-apoptosis ye-signal-regulating kinase 1 (ASK1), ene-anti-inflammatory, i-antineoplastic kunye ne-anti-fibrotic imisebenzi. Iithagethi ze-GS-4997 kwaye zibophelela kwi-catalytic kinase domain ye-ASK1 ngendlela ye-ATP-ekhuphisanayo, ngaloo ndlela ikhusela i-phosphorylation kunye nokusebenza kwayo. I-GS-4997 ikhusela ukuveliswa kwee-cytokines ezivuthayo, i-down-ilawula ukubonakaliswa kwezakhi zofuzo ezibandakanyekayo kwi-fibrosis, icinezela i-apoptosis eninzi kwaye inqanda ukwanda kwamaselula. |
| CPD100603 | MDK36122 | I-MDK36122, eyaziwa ngokuba yi-H-PGDS Inhibitor I, yi-Prostaglandin D Synthase (uhlobo lwe-hematopoietic) Inhibitor. I-MDK36122 ayinalo igama lekhowudi, kwaye ine-CAS#1033836-12-2. Iidijithi ezi-5 zokugqibela zisetyenziselwe igama kunxibelelwano olulula. I-MDK36122 ivimbela ngokukhethiweyo i-HPGDS (IC50s = 0.7 kunye ne-32 nM kwi-enzyme kunye novavanyo lweselula, ngokulandelanayo) kunye nomsebenzi omncinci ngokuchasene ne-enzymes yabantu ehambelanayo L-PGDS, mPGES, COX-1, COX-2, kunye ne-5-LOX. |
| CPD100602 | Tepoxalin | I-Tepoxalin, eyaziwa ngokuba yi-ORF-20485; RWJ-20485; yi-5-lipoxygenase inhibitor enokuthi ifumane unyango lwe-asthma, i-osteoarthritis (OA). I-Tepoxalin inomsebenzi we-vivo inhibitory ngokuchasene ne-COX-1, i-COX-2, kunye ne-5-LOX kwizinja kwi-dosage evunyiweyo yangoku evunyiweyo.I-Tepoxalin inqanda ukuvuvukala kunye nokungasebenzi kakuhle kwe-microvascular okubangelwa yi-irradiation yesisu kwiigundane. I-Tepoxalin iphakamisa umsebenzi we-antioxidant, i-pyrrolidine dithiocarbamate, ekunciphiseni i-tumor necrosis factor alpha-induced apoptosis kwiiseli ze-WEHI 164. |
| CPD100601 | Tenidap | I-Tenidap, eyaziwa ngokuba yi-CP-66248, yi-COX/5-LOX inhibitor kunye ne-cytokine-modulating anti-inflammatory candidate eyayiphantsi kophuhliso nguPfizer njengonyango oluthembisayo lwe-rheumatoid arthritis, kodwa uPfizer wamisa uphuhliso emva kokuvunywa kwentengiso. yi-FDA ngo-1996 ngenxa yetyhefu kunye netyhefu yezintso, eyabalelwa kwi-metabolites yechiza kunye ne-thiophene moiety eyabangela umonakalo we-oxidative. |
| CPD100600 | PF-4191834 | I-PF-4191834 iyiveli, inamandla kwaye ikhetha i-non-redox ye-5-lipoxygenase inhibitor esebenzayo ekudumbeni kunye neentlungu. I-PF-4191834 ibonisa amandla amahle kwi-enzyme- kunye nee-assays ezisekwe kwiseli, kunye nemodeli yegundane yokuvuvukala okukrakra. Iziphumo zovavanyo lwe-Enzyme zibonisa ukuba i-PF-4191834 yi-5-LOX inhibitor enamandla, ene-IC (50) = 229 +/- 20 nM. Ngaphezu koko, ibonise malunga ne-300-fold selectivity ye-5-LOX phezu kwe-12-LOX kunye ne-15-LOX kwaye ibonisa akukho msebenzi malunga ne-cyclooxygenase enzymes. Ukongezelela, i-PF-4191834 inqanda i-5-LOX kwiiseli zegazi lomntu, kunye ne-IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | I-MK-886, eyaziwa ngokuba yi-L 663536, ngumchasi we-leukotriene. Inokwenza oku ngokuthintela i-5-lipoxygenase activating protein (FLAP), ngaloo ndlela inqanda i-5-lipoxygenase (5-LOX), kwaye inokunceda ekuphatheni i-atherosclerosis. I-MK-886 inqanda umsebenzi we-cyclooxygenase-1 kwaye icinezela i-platelet aggregation. I-MK-886 yenza utshintsho kumjikelezo weseli kwaye yandisa i-apoptosis emva konyango lwe-photodynamic kunye ne-hypericin. I-MK-886 iphucula i-tumor necrosis factor-alpha-induced differentiation kunye ne-apoptosis. |
| CPD100598 | L-691816 | I-L 691816 yi-inhibitor enamandla ye-5-LO yokusabela kokubili kwi-vitro kunye noluhlu lweemodeli ze-vivo. |
| CPD100597 | CMI-977 | I-CMI-977, eyaziwa ngokuba yi-LPD-977 kunye ne-MLN-977, i-5-lipoxygenase inhibitor enamandla engenelela ekuveliseni i-leukotrienes kwaye ngoku iphuhliswa kunyango lwe-asthma engapheliyo. I-CMI-977 inqanda i-5-lipoxygenase (i-5-LO) indlela yokuvuvukala kwamaselula ukuvimbela ukuveliswa kwe-leukotrienes, edlala indima ebalulekileyo ekuqaliseni i-asthma ye-bronchial. |
| CPD100596 | CJ-13610 | I-CJ-13610 yi-inhibitor esebenzayo yomlomo ye-5-lipoxygenase (5-LO) . I-CJ-13610 inqanda i-biosynthesis ye-leukotriene B4 kwaye ilawula ukubonakaliswa kwe-IL-6 mRNA kwi-macrophages. Iyasebenza kwiimodeli zangaphambili zentlungu. |
| CPD100595 | BRP-7 | I-BRP-7 yi-5-LO activating protein (FLAP) inhibitor. |
| CPD100594 | TT15 | I-TT15 yi-agonist ye-GLP-1R. |
| CPD100593 | VU0453379 | I-VU0453379 yi-CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric module (PAM) |
