| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100616 | Emricasan | Emricasan, eo hape e tsejoang e le IDN 6556 le PF 03491390, ke "caspase inhibitor" ea pele-pele litekong tsa meriana bakeng sa phekolo ea mafu a sebete. Emricasan (IDN-6556) e fokotsa kotsi ea sebete le fibrosis ka mohlala oa murine oa steatohepatitis e seng joala. IDN6556 e thusa ho kenngoa ha lihlekehleke tse ka thōko ho mofuta oa porcine islet autotransplant. IDN-6556 ea molomo e ka fokotsa ts'ebetso ea aminotransferase ho bakuli ba nang le lefu la sebete le sa foleng la lefu la sebete la C. PF-03491390 e tsamaisoang ka molomo e bolokiloe sebeteng ka nako e telele e nang le ts'oaetso e tlaase ea tsamaiso, e nang le phello ea hepatoprotective khahlanong le kotsi ea sebete e bakoang ke alpha-fas ka mohlala oa mouse. . |
| CPD100615 | Q-VD-Oph | QVD-OPH, eo hape e tsejoang e le Quinoline-Val-Asp-Difluorophenoxymethylketone, ke sephara se sephara sa caspase inhibitor se nang le thepa e matla ea antiapoptotic. Q-VD-OPh e thibela ho otloa ke neonatal ho P7 rat: karolo ea bong. Q-VD-OPh e na le liphello tse khahlanong le leukemia 'me e ka sebelisana le li-analogue tsa vithamine D ho eketsa pontšo ea HPK1 liseleng tsa AML. Q-VD-OPh e fokotsa apoptosis e bakoang ke ho sithabela maikutlo 'me e ntlafatsa ho hlaphoheloa ha setho sa morao-rao ho likhoto ka mor'a kotsi ea mokokotlo. |
| CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk ke cell-permeable, inhibitor e ke keng ea fetoloa ea caspase-3. Caspase-3 ke cysteineyl aspartate-specific protease e bapalang karolo ea mantlha ho apoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, e tsejoang hape e le Z-IETD-FMK, ke inhibitor e matla, e khonang ho kenella ka liseleng, e ke keng ea fetoloa ea caspase-8 le granzyme B., The Caspase-8 Inhibitor II e laola ts'ebetso ea tlhaho ea Caspase-8. MDK4982 e thibela ka katleho apoptosis e bakoang ke kokoana-hloko ea ntaramane liseleng tsa HeLa. MDK4982 e boetse e thibela granzyme B. MDK4982 e na le CAS #210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK ke cell-permeable, e ke keng ea fetoloa ea pan-caspase inhibitor. Z-VAD-FMK e thibela ts'ebetso ea caspase le ho kenngoa ha apoptosis liseleng tsa tumor in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, e tsejoang hape e le VX-765, e etselitsoe ho thibela Caspase, e leng enzyme e laolang tlhahiso ea li-cytokine tse peli, IL-1b le IL-18. VX-765 e bonts'itsoe hore e thibela ho ts'oaroa ho matla mefuteng ea preclinical. Ntle le moo, VX-765 e bonts'itse ts'ebetso mefuteng ea pele ea lefu la sethoathoa se sa foleng. VX-765 e ne e fuoe bakuli ba fetang 100 litekong tsa kliniki tsa phase-I le phase-IIa tse amanang le mafu a mang, ho kenyeletsoa le teko ea kliniki ea matsatsi a 28 ho bakuli ba nang le psoriasis. E phethetse mohato oa phekolo oa teko ea kliniki ea phase-IIa ea VX-765 e ngolisitseng bakuli ba ka bang 75 ba nang le lefu la sethoathoa le hananang le phekolo. Teko ea kliniki e laoloang ka makhetlo a mabeli, e sa tloaelehang, e laoloang ke placebo e ne e etselitsoe ho hlahloba ts'ireletso, mamello le ts'ebetso ea bongaka ea VX-765. |
| CPD100610 | Maraviroc | Maraviroc ke antiviral, e matla, e se nang tlhōlisano ea li-receptor tsa CKR-5 tse thibelang ho tlama ha HIV viral coat protein gp120. Maraviroc e thibela MIP-1β-stimulated γ-S-GTP e tlamang ho HEK-293 lisele tsa lisele, e bontšang bokhoni ba eona ba ho thibela ts'usumetso e itšetlehileng ka chemokine ea phapanyetsano ea GDP-GTP setsing sa protheine sa CKR-5 / G. Maraviroc e boetse e thibela ketsahalo e ka tlase ea noka ea chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Resatorvid | Resatorvid, eo hape e tsejoang e le TAK-242, ke cell-permeable inhibitor ea pontšo ea TLR4, e thibela tlhahiso e entsoeng ke LPS ea NO, TNF-α, IL-6, le IL-1β ka macrophages e nang le IC50 boleng ba 1-11 nM. Resatorvid e tlama TLR4 ka boikhethelo 'me e kena-kenana le litšebelisano lipakeng tsa TLR4 le limolek'hule tsa adaptara ea eona. Resatorvid e fana ka "neuroprotection" tekong ea ts'oaetso e bohloko ea boko: moelelo oa phekolo ea kotsi ea boko ba motho |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 ke inhibitor ea molomo ea bioavailable ea apoptosis signal-regulating kinase 1 (ASK1). E khetha ASK1 ho feta ASK2 hammoho le MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, le B-RAF. E thibela keketseho e bakoang ke streptozotocin ho JNK le p38 phosphorylation ho INS-1 pancreatic β lisele ka mokhoa o itšetlehileng ka mahloriso. |
| CPD100607 | K811 | K811 ke ASK1-specific inhibitor e lelefatsang ho phela ka mokhoa oa toeba oa amyotrophic lateral sclerosis. K811 e ile ea thibela ka katleho ho ata ha lisele meleng ea lisele tse nang le polelo e phahameng ea ASK1 le liseleng tsa GC tsa HER2-overexpressing. Kalafo ka K811 e fokolitse boholo ba lihlahala tsa xenograft ka ho theola matšoao a ho ata. |
| CPD100606 | K812 | K812 ke ASK1-specific inhibitor e fumanoeng ho lelefatsa ho phela ka mokhoa oa toeba oa amyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | MSC 2032964A ke ASK1 inhibitor e matla le e khethang (IC50 = 93 nM). E thibela LPS-induced ASK1 le p38 phosphorylation ho li-astrocyte tsa mouse e hlahisitsoeng le ho hatella neuroinfigueation ka mokhoa oa mouse oa EAE. MSC 2032964A e fumaneha ka molomo ebile e kenella bokong. |
| CPD100604 | Selonsertib | Selonsertib, e tsejoang hape e le GS-4997, ke inhibitor ea molomo ea bioavailable ea apoptosis signal-regulating kinase 1 (ASK1), e nang le mesebetsi e ka bang khahlanong le ho ruruha, anti-antineoplastic le anti-fibrotic. GS-4997 e ipapisa le "catalytic kinase domain" ea ASK1 ka mokhoa oa tlholisano oa ATP, ka hona e thibela phosphorylation le ts'ebetso ea eona. GS-4997 e thibela tlhahiso ea li-cytokine tsa ho ruruha, ho theola-ho laola polelo ea liphatsa tsa lefutso tse amehang ho fibrosis, ho hatella apoptosis e feteletseng le ho thibela ho ata ha lisele. |
| CPD100603 | MDK36122 | MDK36122, e tsejoang hape e le H-PGDS Inhibitor I, ke Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 ha e na lebitso la khoutu, mme e na le CAS#1033836-12-2. Linomoro tse 5 tsa ho qetela li sebelisitsoe bakeng sa lebitso bakeng sa puisano e bonolo. MDK36122 e thibela ka mokhoa o ikhethileng HPGDS (IC50s = 0.7 le 32 nM ka li-enzyme le liteko tsa cellular, ka ho latellana) ka ts'ebetso e nyane khahlano le li-enzyme tse amanang le batho L-PGDS, mPGES, COX-1, COX-2, le 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, e tsejoang hape e le ORF-20485; RWJ-20485; ke 5-lipoxygenase inhibitor e khonang ho phekola asthma, osteoarthritis (OA). Tepoxalin e na le ts'ebetso ea inhibitory ea vivo khahlanong le COX-1, COX-2, le 5-LOX ho lintja ka tekanyo e khothalletsoang ea hona joale e amohelehang.Tepoxalin e thibela ho ruruha le ho se sebetse ha microvascular ho bakoang ke mahlaseli a mpeng ho likhoto. Tepoxalin e ntlafatsa ts'ebetso ea antioxidant, pyrrolidine dithiocarbamate, ho attenuating tumor necrosis factor alpha-induced apoptosis liseleng tsa WEHI 164. |
| CPD100601 | Tenidap | Tenidap, eo hape e tsejoang e le CP-66248, ke COX/5-LOX inhibitor le cytokine-modulating anti-inflammatory inhibitor e neng e ntse e ntlafatsoa ke Pfizer e le pheko e ts'episang bakeng sa ramatiki ea ramatiki, empa Pfizer o ile a emisa nts'etsopele kamora hore tumello ea papatso e haneloe. ke FDA ka 1996 ka lebaka la chefo ea sebete le liphio, e neng e bakoa ke metabolites ea moriana o nang le karolo ea thiophene e bakileng tšenyo ea oxidative. |
| CPD100600 | PF-4191834 | PF-4191834 ke buka, e matla le e khethollang e seng redox 5-lipoxygenase inhibitor e sebetsang ho ruruha le bohloko. PF-4191834 e bonts'a potency e ntle litekong tsa enzyme- le liseleng, hammoho le mohlala oa likhoto oa ho ruruha ho matla. Liphetho tsa tlhahlobo ea enzyme li bontša hore PF-4191834 ke 5-LOX inhibitor e matla, e nang le IC(50) = 229 +/- 20 nM. Ho feta moo, e bontšitse hoo e batlang e le 300-fold selectivity bakeng sa 5-LOX holim'a 12-LOX le 15-LOX 'me e bontša ha ho mosebetsi o lebisang ho li-enzyme tsa cyclooxygenase. Ho phaella moo, PF-4191834 e thibela 5-LOX liseleng tsa mali tsa motho, tse nang le IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, eo hape e tsejoang e le L 663536, ke mohanyetsi oa leukotriene. E ka etsa sena ka ho thibela 5-lipoxygenase activating protein (FLAP), kahoo e thibela 5-lipoxygenase (5-LOX), 'me e ka thusa ho phekola atherosclerosis. MK-886 e thibela ts'ebetso ea cyclooxygenase-1 mme e hatella platelet aggregation. MK-886 e etsa hore ho be le liphetoho ka potoloho ea lisele 'me e eketsa apoptosis ka mor'a phekolo ea photodynamic e nang le hypericin. MK-886 e ntlafatsa phapang ea tumor necrosis factor-alpha-induced le apoptosis. |
| CPD100598 | L-691816 | L 691816 ke inhibitor e matla ea 5-LO reaction ka bobeli in vitro le mefuta e mengata ea in vivo. |
| CPD100597 | CMI-977 | CMI-977, eo hape e tsejoang e le LPD-977 le MLN-977, ke inhibitor e matla ea 5-lipoxygenase e kenellang tlhahisong ea li-leukotrienes 'me e ntse e ntlafatsoa bakeng sa phekolo ea asthma e sa foleng. CMI-977 e thibela 5-lipoxygenase (5-LO) tsela ea ho ruruha ea cellular ho thibela moloko oa leukotrienes, o phethang karolo ea bohlokoa ho bakang asthma ea bronchial. |
| CPD100596 | CJ-13610 | CJ-13610 ke inhibitor e sebetsang ka molomo ea 5-lipoxygenase (5-LO) . CJ-13610 e thibela biosynthesis ea leukotriene B4 mme e laola polelo ea IL-6 mRNA ho macrophages. E sebetsa hantle mefuteng ea pele ea bohloko. |
| CPD100595 | BRP-7 | BRP-7 ke 5-LO activating protein (FLAP) inhibitor. |
| CPD100594 | TT15 | TT15 ke agonist ea sehlopha sa GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 ke CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) |
