| CAT # | Inoa Huahana | wehewehe |
| CPD100616 | Emricasan | ʻO Emricasan, ka mea i ʻike ʻia ʻo IDN 6556 a me PF 03491390, he mea hoʻopiʻi caspase papa mua i nā hoʻokolohua lapaʻau no ka mālama ʻana i nā maʻi ate. Hoʻemi ʻo Emricasan (IDN-6556) i ka hōʻeha o ka ate a me ka fibrosis i loko o kahi hiʻohiʻona murine o ka steatohepatitis non-alcoholic. Hoʻomaʻamaʻa ʻo IDN6556 i ka hoʻopili ʻana i nā mokupuni liʻiliʻi ma kahi kumu hoʻohālike autotransplant puaʻa. Hiki i ka waha IDN-6556 ke hoʻohaʻahaʻa i ka hana aminotransferase i nā poʻe maʻi me ka maʻi hepatitis C. Hoʻopaʻa ʻia ʻo PF-03491390 i loko o ke akepaʻa no nā manawa lōʻihi me ka haʻahaʻa haʻahaʻa o ka ʻōnaehana, e hana ana i kahi hopena hepatoprotective e kūʻē i ka hōʻeha ate alpha-fas-induced i loko o kahi kiʻi kiʻi. . |
| CPD100615 | Q-VD-Oph | ʻO QVD-OPH, ka mea i kapa ʻia ʻo Quinoline-Val-Asp-Difluorophenoxymethylketone, he mea hoʻopiʻi caspase ākea ākea me nā waiwai antiapoptotic ikaika. Kāohi ʻo Q-VD-OPh i ka hahau neonatal i ka ʻiole P7: he kuleana no ke kāne. Loaʻa i ka Q-VD-OPh nā hopena anti-leukemia a hiki ke launa pū me nā analogs vitamin D e hoʻonui i ka hōʻailona HPK1 i nā pūnaewele AML. Hoʻemi ʻo Q-VD-OPh i ka apoptosis i hoʻoulu ʻia i ka trauma a hoʻomaikaʻi i ka hoʻihoʻi ʻana o ka hana hope-lima i nā ʻiole ma hope o ka hōʻeha ʻana i ke kuamoʻo. |
| CPD100614 | Z-DEVD-FMK | ʻO Z-DEVD-fmk kahi mea paʻa i ka cell-permeable, hiki ʻole ke hoʻohuli ʻia o ka caspase-3. ʻO Caspase-3 kahi protease kikoʻī cysteinyl aspartate e pāʻani ana i kahi koʻikoʻi i ka apoptosis. |
| CPD100613 | Z-IETD-FMK | ʻO MDK4982, ka mea i kapa ʻia ʻo Z-IETD-FMK, he mea hoʻopaneʻe ikaika, cell-permeable, hiki ʻole ke hoʻololi ʻia o ka caspase-8 a me ka granzyme B., Na ka Caspase-8 Inhibitor II e hoʻomalu i ka hana biological o Caspase-8. Kāohi maikaʻi ʻo MDK4982 i ka apoptosis i hoʻokomo ʻia i ka maʻi maʻi influenza i nā cell HeLa. Kāohi pū ʻo MDK4982 i ka granzyme B. Loaʻa iā MDK4982 CAS #210344-98-2. |
| CPD100612 | Z-VAD-FMK | ʻO Z-VAD-FMK kahi mea hoʻopaneʻe pan-caspase hiki ke hoʻololi. Hoʻopaʻa ʻo Z-VAD-FMK i ka hana caspase a me ka hoʻokomo ʻana o ka apoptosis i loko o nā pūnaewele tumor in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belenacasan | ʻO Belnacasan, ka mea i kapa ʻia ʻo VX-765, ua hoʻolālā ʻia e kāohi i ka Caspase, ʻo ia ka enzyme e hoʻomalu i ka hana o ʻelua cytokines, IL-1b a me IL-18. Ua hōʻike ʻia ʻo VX-765 e kāohi i ka hopu ʻana i ka maʻi ma nā ʻano preclinical. Eia kekahi, ua hōʻike ʻo VX-765 i ka hana ma nā hiʻohiʻona preclinical o ka epilepsy maʻi. Ua kau ʻia ʻo VX-765 ma luna o 100 mau mea maʻi ma ka pae-I a me ka phase-IIa hoʻāʻo lapaʻau e pili ana i nā maʻi ʻē aʻe, me ka hoʻāʻo hoʻokolohua 28-lā phase-IIa i nā maʻi me psoriasis. Ua hoʻopau ʻo ia i ka lāʻau lapaʻau o kahi hoʻokolohua lapaʻau phase-IIa o VX-765 i hoʻopaʻa inoa ma kahi o 75 mau maʻi me ka maʻi epilepsy kūpaʻa. Ua hoʻolālā ʻia ka hoʻokolohua lapaʻau pālua-makapō, randomized, placebo-controlled clinical trial no ka loiloi i ka palekana, ka hoʻomanawanui a me ka hana lapaʻau o VX-765. |
| CPD100610 | ʻO Maraviroc | ʻO Maraviroc kahi antiviral, potent, non-competitive CKR-5 receptor antagonist e pale ana i ka hoʻopaʻa ʻana o ka HIV viral coat protein gp120. Hoʻopaʻa ʻo Maraviroc i ka MIP-1β-stimulated γ-S-GTP i hoʻopaʻa ʻia i nā membrane cell HEK-293, e hōʻike ana i kona hiki ke kāohi i ka chemokine-dependent stimulation o GDP-GTP exchange ma ka CKR-5 / G protein complex. Hoʻopaʻa pū ʻo Maraviroc i ka hanana i lalo o ka chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Restatorvid | ʻO Restatorvid, ka mea i kapa ʻia ʻo TAK-242, he mea hoʻopio cell-permeable o ka hōʻailona TLR4, ke kāohi nei i ka hana LPS-i hoʻokomo ʻia o NO, TNF-α, IL-6, a me IL-1β i nā macrophages me nā waiwai IC50 o 1-11 nM. Hoʻopili paʻa ʻo Restatorvid iā TLR4 a keʻakeʻa i nā pilina ma waena o TLR4 a me kāna mau molekele adapter. Hāʻawi ʻo Restatorvid i ka neuroprotection i ka ʻeha ʻeha o ka lolo traumatic: implication i ka mālama ʻana i ka ʻeha lolo kanaka |
| CPD100608 | ASK1-Inhibitor-10 | ʻO ka ASK1 Inhibitor 10 he mea hoʻopaneʻe waha bioavailable o ka apoptosis hōʻailona-hoʻoponopono kinase 1 (ASK1). He koho ia no ASK1 ma luna o ASK2 a me MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, a me B-RAF. Kāohi ia i ka piʻi ʻana o ka streptozotocin-induced i ka JNK a me ka p38 phosphorylation i loko o INS-1 pancreatic β cell ma kahi ʻano hilinaʻi. |
| CPD100607 | K811 | ʻO K811 kahi mea hoʻopaneʻe kikoʻī ASK1 e hoʻolōʻihi i ke ola ʻana i kahi ʻano ʻiole o ka amyotrophic lateral sclerosis. Kāohi maikaʻi ʻo K811 i ka hoʻonui ʻana o ke kelepona ma nā laina kelepona me ka hōʻike ASK1 kiʻekiʻe a ma nā pūnaewele GC-overexpressing HER2. ʻO ka lapaʻau ʻana me K811 i hoʻemi ʻia ka nui o nā maʻi maʻi xenograft ma o ka hoʻohaʻahaʻa ʻana i nā hōʻailona proliferation. |
| CPD100606 | K812 | ʻO K812 kahi mea hoʻopaneʻe kikoʻī ASK1 i ʻike ʻia e hoʻolōʻihi i ke ola ʻana i kahi ʻano ʻiole o ka amyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | ʻO MSC 2032964A kahi mea hoʻokae ASK1 ikaika a koho (IC50 = 93 nM). Hoʻopaʻa ia i ka LPS-induced ASK1 a me ka p38 phosphorylation i nā astrocytes ʻiole moʻomeheu a hoʻopau i ka neuroinflammation i kahi kiʻi EAE kiʻi. ʻO MSC 2032964A ka mea hiki ke loaʻa i ka waha a me ka lolo. |
| CPD100604 | Selonsertib | ʻO Selonsertib, ka mea i kapa ʻia ʻo GS-4997, he mea hoʻopiʻi waha bioavailable o ka apoptosis signal-regulating kinase 1 (ASK1), me nā hana anti-inflammatory, antineoplastic a me nā hana anti-fibrotic. ʻO GS-4997 nā pahuhopu a hoʻopaʻa i ka catalytic kinase domain o ASK1 ma kahi ʻano hoʻokūkū ATP, no laila e pale ai i kāna phosphorylation a me ka hoʻāla ʻana. Kāohi ʻo GS-4997 i ka hana ʻana o nā cytokine inflammatory, hoʻoponopono i ka hōʻike ʻana o nā genes i komo i ka fibrosis, hoʻopau i ka apoptosis nui a keʻakeʻa i ka hoʻonui ʻana o ka cellular proliferation. |
| CPD100603 | MDK36122 | ʻO MDK36122, i kapa ʻia ʻo H-PGDS Inhibitor I, he Prostaglandin D Synthase (hematopoietic-type) Inhibitor. ʻAʻohe inoa code MDK36122, a he CAS #1033836-12-2. Ua hoʻohana ʻia ka helu 5 hope loa no ka inoa no ke kamaʻilio maʻalahi. MDK36122 koho i ka HPGDS (IC50s = 0.7 a me 32 nM i ka enzyme a me ka cellular assays, i kēlā me kēia) me ka hana liʻiliʻi e kūʻē i nā enzymes kanaka pili L-PGDS, mPGES, COX-1, COX-2, a me 5-LOX. |
| CPD100602 | Tepoxalin | ʻO Tepoxalin, i kapa ʻia ʻo ORF-20485; RWJ-20485; he 5-lipoxygenase inhibitor hiki ke mālama i ka hānō, osteoarthritis (OA). Loaʻa i ka Tepoxalin i loko o ka vivo ka hana hoʻoneʻe kūʻē iā COX-1, COX-2, a me 5-LOX i nā ʻīlio ma ke ʻano i ʻae ʻia i kēia manawa. Hoʻonui ʻo Tepoxalin i ka hana o kahi antioxidant, pyrrolidine dithiocarbamate, i ka attenuating tumor necrosis factor alpha-induced apoptosis ma WEHI 164 cell. |
| CPD100601 | Tenidap | ʻO Tenidap, ka mea i kapa ʻia ʻo CP-66248, he mea hoʻopaʻa COX/5-LOX a me ka cytokine-modulating anti-inflammatory moho lāʻau i hoʻomohala ʻia e Pfizer ma ke ʻano he lāʻau lapaʻau kūpono no ka rheumatoid arthritis, akā ua hoʻōki ʻo Pfizer i ka hoʻomohala ʻana ma hope o ka hōʻole ʻia ʻana o ka ʻae kūʻai. e ka FDA i ka makahiki 1996 ma muli o ka make o ka ate a me ka puʻupaʻa, i pili i nā metabolites o ka lāʻau lapaʻau me kahi thiophene moiety. ka mea i poino oxidative. |
| CPD100600 | PF-4191834 | ʻO ka PF-4191834 he puke moʻolelo, ikaika a koho ʻole ʻia ka non-redox 5-lipoxygenase inhibitor kūpono i ka mumū a me ka ʻeha. Hōʻike ʻo PF-4191834 i ka mana maikaʻi i ka enzyme-a me ka cell-based assays, a me ke ʻano hoʻohālike o ka ʻiole o ka ʻeha nui. Hōʻike nā hopena hoʻokolohua Enzyme ʻo PF-4191834 he mea hoʻopale 5-LOX ikaika, me kahi IC(50) = 229 +/- 20 nM. Eia kekahi, ua hōʻike ʻia ma kahi o 300-fold selectivity no 5-LOX ma luna o 12-LOX a me 15-LOX a ʻaʻole hōʻike i kahi hana e pili ana i nā enzyme cyclooxygenase. Eia hou, PF-4191834 kaohi i ka 5-LOX i loko o ke koko koko kanaka, me ka IC(80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | ʻO MK-886, i ʻike ʻia ʻo L 663536, he mea kūʻē leukotriene. Hiki iā ia ke hana i kēia ma ke kāohi ʻana i ka 5-lipoxygenase activating protein (FLAP), no laila ke kāohi ʻana i ka 5-lipoxygenase (5-LOX), a hiki ke kōkua i ka mālama ʻana i ka atherosclerosis. Kāohi ʻo MK-886 i ka hana cyclooxygenase-1 a hoʻopaʻa i ka platelet aggregation. Hoʻokomo ʻo MK-886 i nā loli i ka pōʻai cell a hoʻonui i ka apoptosis ma hope o ka photodynamic therapy me hypericin. Hoʻonui ka MK-886 i ka ʻokoʻa o ka necrosis factor-alpha-induced apoptosis. |
| CPD100598 | L-691816 | ʻO L 691816 kahi mea hoʻopaneʻe ikaika o ka hopena 5-LO i loko o ka vitro a i loko o kahi ʻano o nā hiʻohiʻona in vivo. |
| CPD100597 | CMI-977 | ʻO CMI-977, ʻike pū ʻia ʻo LPD-977 a me MLN-977, he mea hoʻopaneʻe 5-lipoxygenase ikaika e komo i ka hana ʻana o nā leukotrienes a ke kūkulu ʻia nei no ka mālama ʻana i ka hānō mau loa. Kāohi ʻo CMI-977 i ka 5-lipoxygenase (5-LO) cellular inflammation ala e ālai ai i ka hana o nā leukotrienes, kahi mea nui i ka hoʻoulu ʻana i ka hānō bronchial. |
| CPD100596 | CJ-13610 | ʻO CJ-13610 kahi mea hoʻokae waha o 5-lipoxygenase (5-LO) . Kāohi ʻo CJ-13610 i ka biosynthesis o leukotriene B4 a hoʻoponopono i ka ʻōlelo IL-6 mRNA i nā macrophages. He kūpono ia i nā ʻano preclinical o ka ʻeha. |
| CPD100595 | BRP-7 | ʻO BRP-7 kahi mea hoʻokae 5-LO activating protein (FLAP). |
| CPD100594 | TT15 | ʻO TT15 kahi agonist o ka GLP-1R. |
| CPD100593 | VU0453379 | ʻO VU0453379 kahi CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) |
