| CAT # | Ingoa Hua | Whakaahuatanga |
| CPD100616 | Emricasan | Ko Emricasan, e mohiotia ana ko te IDN 6556 me te PF 03491390, he kaiwawao caspase tuatahi i roto i te akomanga i roto i nga whakamatautau haumanu mo te maimoatanga o nga mate ate. Ko te Emricasan (IDN-6556) ka whakaheke i te whara ate me te fibrosis i roto i te tauira murine o te steatohepatitis kore-waipiro. Ko te IDN6556 e whakahaere ana i te whakairo o te motu papatipu tawhē i roto i te tauira whakawhiti aunoa o te motu porcine. Ka taea e Oral IDN-6556 te whakaheke i te mahi aminotransferase i roto i nga turoro me te mate hepatitis C. Ko te PF-03491390 te whakahaere-waha ka mau ki roto i te ate mo nga wa roa me te iti o te whakamaanga o te punaha, ka tukuna he paanga hepatoprotective ki te whara ate alpha-fas i roto i te tauira kiore . |
| CPD100615 | Q-VD-Oph | Ko te QVD-OPH, e mohiotia ana ko Quinoline-Val-Asp-Difluorophenoxymethylketone, he aukati caspase whanui whanui me nga taonga antiapoptotic kaha. Ko te Q-VD-OPh te aukati i te whiu whanau hou i roto i te kiore P7: he mahi mo te ira tangata. Kei a Q-VD-OPh nga paanga anti-reukemia, ka taea e ia te taunekeneke me nga tairitenga huaora D hei whakanui ake i te tohu HPK1 i roto i nga pūtau AML. Ko te Q-VD-OPh he whakaheke i te apoptosis i puta mai i te whara me te whakapai ake i te whakaora o te mahi hid-limm i roto i nga kiore i muri i te whara o te taurakira. |
| CPD100614 | Z-DEVD-FMK | Ko te Z-DEVD-fmk he pūtau-permeable, aukati korekore o te caspase-3. Ko te Caspase-3 he protease motuhake-a-cysteinyl aspartate e whai waahi nui ana ki te apoptosis. |
| CPD100613 | Z-IETD-FMK | Ko te MDK4982, e mohiotia ana ko Z-IETD-FMK, he kaha, he pukoro-permeable, he aukati korekore o te caspase-8 me te granzyme B., Ko te Caspase-8 Inhibitor II te whakahaere i te mahi koiora o Caspase-8. Ko te MDK4982 ka taea te aukati i te apoptosis a te huaketo rewharewha i roto i nga pūtau HeLa. Ko te MDK4982 he aukati i te granzyme B. Kei a MDK4982 he CAS#210344-98-2. |
| CPD100612 | Z-VAD-FMK | Ko te Z-VAD-FMK he pūtau-permeable, he aukati pan-caspase e kore e taea te huri. Ko te Z-VAD-FMK ka whakakore i te tukatuka caspase me te whakauru apoptosis i roto i nga pukupuku pukupuku i roto i te vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Peretana | Ko Belnacasan, e mohiotia ana ko VX-765, i hangaia hei aukati i te Caspase, he enzyme e whakahaere ana i te whakatipuranga o nga cytokines e rua, IL-1b me IL-18. Kua whakaatuhia te VX-765 ki te aukati i nga hopukanga whakapeka i roto i nga tauira preclinical. I tua atu, kua whakaatu a VX-765 i nga mahi i roto i nga tauira o mua o te mate pukupuku tawhito. Ko te VX-765 i werohia ki runga i te 100 nga turoro i te wahanga-I me te wahanga-IIa nga whakamatautau haumanu e pa ana ki etahi atu mate, tae atu ki te whakamatautau haumanu 28-ra-IIa i nga turoro me te psoriasis. Kua oti i a ia te waahi maimoatanga o te wahanga-IIa whakamatautau haumanu o VX-765 i whakauru atu ki te 75 nga turoro me te mate rewharewha-atete. Ko te whakamatautau haumanu mata-rua, matapōkeretia, e whakahaerehia ana e te placebo hei arotake i te haumarutanga, te pai me te mahi haumanu o VX-765. |
| CPD100610 | Maraviroc | Ko te Maraviroc he kaitukino, he kaha, he kore-whakataetae CKR-5 kaiwhakawhanake antagonist e aukati ana i te herenga o te koti mate HIV pūmua gp120. Ka whakakorehia e Maraviroc te MIP-1β-stimulated γ-S-GTP e herea ana ki te HEK-293 membranes pūtau, e whakaatu ana i tona kaha ki te whakakore i te whakaongaonga chemokine-ti'aturi o te whakawhitinga GDP-GTP i te CKR-5 / G protein complex. Ka aukati ano a Maraviroc i te kaupapa o raro o te tohatoha o te konupūmā intracellular i roto i te chemokine. |
| CPD100609 | Resatorvid | Ko Resatorvid, e mohiotia ana ko TAK-242, ko te kaitautoko-a-rorohiko o te tohu TLR4, e aukati ana i te hangahanga a te LPS o NO, TNF-α, IL-6, me IL-1β i roto i nga macrophages me nga uara IC50 o 1-11 nM. Ka herea a Restatorvid ki te TLR4 ka pokanoa ki nga taunekeneke i waenga i te TLR4 me ona ngota ngota urutau. Ko te Restatorvid e whakarato ana i te neuroprotection i roto i te whakamatautau i te whara o te roro o te roro: te tikanga mo te maimoatanga o te whara o te roro tangata |
| CPD100608 | ASK1-Aue-10 | Ko te ASK1 Inhibitor 10 he aukati koiora-a-waha mo te apoptosis tohu-whakahaere kinase 1 (ASK1). He mea whiriwhiri mo ASK1 mo ASK2 me MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, me B-RAF. Ka whakakorehia e te streptozotocin te whakanui ake i te JNK me te p38 phosphorylation i roto i nga pūtau β pancreatic INS-1 i roto i te ahua o te kukū. |
| CPD100607 | K811 | Ko te K811 he aukati ASK1-motuhake e whakaroa ana i te oranga i roto i te tauira kiore o te amyotrophic lateral sclerosis. He pai te aukati a K811 i te tipu o te pūtau i roto i nga raina pūtau me te whakapuaki ASK1 teitei me nga pūtau GC-HER2-overexpressing. Ko te maimoatanga me te K811 kua whakahekehia te rahi o nga pukupuku xenograft ma te whakaheke i nga tohu whakahiato. |
| CPD100606 | K812 | Ko te K812 he aukati ASK1-motuhake i kitea hei whakaroa i te oranga i roto i te tauira kiore o te amyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | Ko te MSC 2032964A he kaha me te whiriwhiri i te aukati ASK1 (IC50 = 93 nM). Ka aukatihia e te LPS te ASK1 me te p38 phosphorylation i roto i nga astrocytes kiore whakatipu me te whakakore i te neuroinflammation i roto i te tauira EAE kiore. Ko te MSC 2032964A kei te waatea-a-waha me te uru ki te roro. |
| CPD100604 | Selonsertib | Ko Selonsertib, e mohiotia ana ko GS-4997, he aukati koiora o te apoptosis tohu-whakahaere kinase 1 (ASK1), me nga mahi anti-inflammatory, antineoplastic me te anti-fibrotic. Ko te GS-4997 te whaainga me te herea ki te rohe catalytic kinase o ASK1 i roto i te whakataetae ATP, na reira ka aukati i tana phosphorylation me te whakahohe. Ko te GS-4997 te aukati i te hanga o nga cytokines inflammatory, te whakaheke-whakahaere i te whakaaturanga o nga ira e uru ana ki te fibrosis, te aukati i te apoptosis nui me te aukati i te tipu o te pūtau. |
| CPD100603 | MDK36122 | Ko te MDK36122, e mohiotia ana ko H-PGDS Inhibitor I, he Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 karekau he ingoa waehere, he CAS#1033836-12-2. Ko te 5-mati whakamutunga i whakamahia hei ingoa mo te ngawari o te whakawhitiwhiti korero. Ko te MDK36122 he aukati i te HPGDS (IC50s = 0.7 me te 32 nM i roto i nga whakamaarama me nga whakamatautau pūtau, ia) me te iti o te mahi ki te taha o nga enzymes tangata L-PGDS, mPGES, COX-1, COX-2, me 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, e mohiotia ana ko ORF-20485; RWJ-20485; he aukati 5-lipoxygenase pea mo te maimoatanga o te mate huango, osteoarthritis (OA). Tepoxalin he in vivo mahi aukati ki COX-1, COX-2, me te 5-LOX i roto i nga kuri i te inenga kua whakaaetia o naianei.Ka whakakorehia e te Tepoxalin te mumura me te ngoikoretanga o te microvascular na te irradiation puku i roto i nga kiore. Ka whakanui ake te Tepoxalin i te mahi o te antioxidant, pyrrolidine dithiocarbamate, ki te whakaiti i te take necrosis pukupuku alpha-induced apoptosis i roto i nga pūtau WEHI 164. |
| CPD100601 | Tenidap | Ko Tenidap, e mohiotia ana ko CP-66248, he kaiwhakahau COX/5-LOX me te kaitono tarukino anti-inflammatory cytokine-modulating i raro i te whakawhanaketanga e Pfizer hei rongoa pai mo te mate rūmātiki, engari i aukati a Pfizer i te whakawhanaketanga i muri i te whakahēnga o te whakaaetanga hokohoko. na te FDA i te tau 1996 na te paitini o te ate me te whatukuhu, i kiia ko nga metabolites o te raau taero me te thiophene moiety na te kino o te oxidative. |
| CPD100600 | PF-4191834 | Ko te PF-4191834 he pukapuka, he kaha me te whiriwhiri kore-redox 5-lipoxygenase inhibitor e whai hua ana ki te mumura me te mamae. Ko te PF-4191834 e whakaatu ana i te kaha pai i roto i nga whakawaehere-a-a-puutau, me te tauira kiore o te mumura whakapeka. Ko nga hua o te whakamatautau i te Enzyme e tohu ana ko te PF-4191834 he aukati 5-LOX kaha, me te IC(50) = 229 +/- 20 nM. I tua atu, i whakaatu tata ki te 300-fold te whiriwhiringa mo te 5-LOX i runga i te 12-LOX me te 15-LOX me te kore e whakaatu he mahi ki nga enzymes cyclooxygenase. I tua atu, ka whakakorehia e te PF-4191834 te 5-LOX i roto i nga ruma toto tangata, me te IC(80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | Ko MK-886, e mohiotia ana ko L 663536, he kaitukino leukotriene. Ka mahia tenei ma te aukati i te 5-lipoxygenase activating protein (FLAP), ka aukati i te 5-lipoxygenase (5-LOX), ka awhina pea ki te rongoa i te atherosclerosis. Ko te MK-886 te aukati i te mahi cyclooxygenase-1 me te whakakore i te whakahiato pereti. Ko te MK-886 e whakaohooho ana i nga huringa o te huringa pūtau me te whakanui ake i te apoptosis i muri i te whakamaaramatanga photodynamic me te hypericin. Ko te MK-886 te whakanui ake i te mate pukupuku mate-a-alpha-induced differentiation and apoptosis. |
| CPD100598 | L-691816 | Ko L 691816 he aukati kaha o te tauhohenga 5-LO i roto i te vitro me te awhe o nga tauira in vivo. |
| CPD100597 | CMI-977 | Ko te CMI-977, e mohiotia ana ko LPD-977 me MLN-977, he aukati 5-lipoxygenase kaha e wawao ana ki te hanga leukotrienes, a kei te whakawhanakehia inaianei mo te maimoatanga o te mate huango mau tonu. Ka aukati te CMI-977 i te ara mumura o te 5-lipoxygenase (5-LO) ki te aukati i te whakatipuranga o nga leukotrienes, e whai waahi nui ana ki te whakaoho i te mate huango. |
| CPD100596 | CJ-13610 | Ko te CJ-13610 he aukati kaha-waha o te 5-lipoxygenase (5-LO) . Ka whakakorehia e CJ-13610 te koiora o te leukotriene B4 me te whakahaere i te whakaaturanga IL-6 mRNA i roto i nga macrophages. He whai hua i roto i nga tauira o mua o te mamae. |
| CPD100595 | BRP-7 | Ko te BRP-7 he 5-LO activating protein (FLAP) aukati. |
| CPD100594 | TT15 | Ko te TT15 he agonist o te GLP-1R. |
| CPD100593 | VU0453379 | Ko te VU0453379 he kaikawe peptide 1 rite ki te glucagon-penetrant CNS (GLP-1R) (GLP-1R) totika allosteric modulator (PAM) |
