| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD100616 | Emricasan | Emricasan, wanda kuma aka sani da IDN 6556 da PF 03491390, shine mai hanawar caspase na farko a cikin gwaji na asibiti don maganin cututtukan hanta. Emricasan (IDN-6556) yana rage raunin hanta da fibrosis a cikin samfurin murine na steatohepatitis mara giya. IDN6556 yana sauƙaƙa da haɓakar ɗimbin tsibiri a cikin ƙirar tsibiri autotransplant. IDN-6556 na baka na iya rage aikin aminotransferase a cikin marasa lafiya tare da ciwon hanta na kullum. PF-03491390 da aka sarrafa ta baki yana riƙe da hanta na tsawon lokaci tare da ƙananan bayyanar cututtuka, yana haifar da sakamako na hepatoprotective akan alpha-fas-induced hanta rauni a cikin wani linzamin kwamfuta model. . |
| Saukewa: CPD100615 | Q-VD-Oph | QVD-OPH, wanda kuma aka sani da Quinoline-Val-Asp-Difluorophenoxymethylketone, babban inhibitor caspase mai faɗi tare da kaddarorin antiapoptotic masu ƙarfi. Q-VD-OPh yana hana bugun jini na jariri a cikin P7 bera: rawar da jinsi. Q-VD-OPh yana da tasirin cutar sankarar bargo kuma yana iya hulɗa tare da analogs na bitamin D don haɓaka siginar HPK1 a cikin ƙwayoyin AML. Q-VD-OPh yana rage apoptosis da ke haifar da rauni kuma yana inganta dawo da aikin hind-gama a cikin berayen bayan rauni na kashin baya. |
| Saukewa: CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk shine tantanin halitta, mai hanawa na caspase-3. Caspase-3 shine cysteinyl aspartate takamaiman protease wanda ke taka muhimmiyar rawa a cikin apoptosis. |
| Saukewa: CPD100613 | Z-IETD-FMK | MDK4982, wanda kuma aka sani da Z-IETD-FMK, mai ƙarfi ne, mai iya jurewa, mai hanawa na caspase-8 da granzyme B., Caspase-8 Inhibitor II yana sarrafa ayyukan nazarin halittu na Caspase-8. MDK4982 yadda ya kamata yana hana apoptosis mai haifar da mura a cikin ƙwayoyin HeLa. MDK4982 kuma yana hana granzyme B. MDK4982 yana da CAS # 210344-98-2. |
| Saukewa: CPD100612 | Z-VAD-FMK | Z-VAD-FMK mai iya jurewa tantanin halitta, mai hana pan-caspase wanda ba zai iya jurewa ba. Z-VAD-FMK yana hana aikin caspase da shigar da apoptosis a cikin ƙwayoyin tumor a cikin vitro (IC50 = 0.0015 - 5.8 mM). |
| Saukewa: CPD100611 | Belnacasan | Belnacasan, wanda aka fi sani da VX-765, an tsara shi don hana Caspase, wanda shine enzyme wanda ke kula da tsararrun cytokines guda biyu, IL-1b da IL-18. An nuna VX-765 don hana tsangwama a cikin ƙididdiga na asali. Bugu da kari, VX-765 ya nuna aiki a cikin preclinical model na kullum epilepsy. An yi amfani da VX-765 a cikin marasa lafiya fiye da 100 a cikin lokaci-I da na lokaci-IIa gwaji na asibiti da suka shafi wasu cututtuka, ciki har da gwajin gwaji na kwanaki 28-IIa a cikin marasa lafiya tare da psoriasis. Ya kammala lokacin jiyya na gwaji na asibiti na kashi-IIa na VX-765 wanda ya yi rajista kusan marasa lafiya 75 da farfadiya mai jure jiyya. An tsara gwajin makafi biyu, bazuwar, gwajin gwaji na asibiti don kimanta aminci, haƙuri da aikin asibiti na VX-765. |
| Saukewa: CPD100610 | Maraviroc | Maraviroc antiviral ne, mai ƙarfi, mara gasa CKR-5 antagonist mai karɓa wanda ke hana ɗaure furotin rigar kwayar cutar HIV gp120. Maraviroc ya hana MIP-1β-stimulated γ-S-GTP daure zuwa HEK-293 membranes cell membranes, yana nuna ikonsa na hana chemokine-dogara stimulating na GDP-GTP musayar a CKR-5/G gina jiki hadaddun. Maraviroc kuma yana hana abubuwan da ke faruwa a ƙasa na sake rarraba calcium cikin salula na chemokine. |
| Saukewa: CPD100609 | Resatorvid | Resatorvid, wanda kuma aka sani da TAK-242, shine mai hanawa ta tantanin halitta na siginar TLR4, yana hana samar da LPS na NO, TNF-α, IL-6, da IL-1β a cikin macrophages tare da ƙimar IC50 na 1-11 nM. Resatorvid yana ɗaure zaɓaɓɓu zuwa TLR4 kuma yana tsangwama tare da hulɗar tsakanin TLR4 da ƙwayoyin adaftar sa. Resatorvid yana ba da kariya ga neuroprotection a cikin raunin kwakwalwa na gwaji: tasiri a cikin maganin raunin kwakwalwar ɗan adam |
| Saukewa: CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 shine mai hanawa na baka mai hanawa na siginar apoptosis mai daidaita kinase 1 (ASK1). Yana da zaɓi don ASK1 akan ASK2 haka kuma MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, da B-RAF. Yana hana haɓakar streptozotocin a cikin JNK da p38 phosphorylation a cikin ƙwayoyin β na pancreatic na INS-1 a cikin hanyar dogaro da hankali. |
| Saukewa: CPD100607 | K811 | K811 shine takamaiman mai hanawa ASK1 wanda ke tsawaita rayuwa a cikin ƙirar linzamin kwamfuta na amyotrophic lateral sclerosis. K811 da kyau ya hana yaduwar kwayar halitta a cikin layin salula tare da babban maganganun ASK1 kuma a cikin HER2-overexpressing GC Kwayoyin. Jiyya tare da K811 ya rage girman ciwace-ciwacen ciwace-ciwacen daji ta hanyar raguwar alamomin yaduwa. |
| Saukewa: CPD100606 | K812 | K812 shine takamaiman mai hanawa ASK1 wanda aka gano don tsawaita rayuwa a cikin ƙirar linzamin kwamfuta na amyotrophic lateral sclerosis. |
| Saukewa: CPD100605 | Saukewa: MSC-2032964A | MSC 2032964A mai ƙarfi ne kuma mai hanawa ASK1 (IC50 = 93 nM). Yana toshe LPS-induced ASK1 da p38 phosphorylation a cikin al'ada linzamin kwamfuta astrocytes da kuma kashe neuroinflammation a cikin wani linzamin kwamfuta model EAE. MSC 2032964A abu ne mai yiwuwa a baka kuma yana shiga kwakwalwa. |
| Saukewa: CPD100604 | Selonsertib | Selonsertib, wanda kuma aka sani da GS-4997, shine mai hanawa na baka mai hanawa na siginar apoptosis mai sarrafa kinase 1 (ASK1), tare da yuwuwar rigakafin kumburi, antineoplastic da ayyukan anti-fibrotic. GS-4997 yana hari kuma yana ɗaure zuwa yankin kinase na catalytic na ASK1 a cikin hanyar gasa ta ATP, ta haka yana hana phosphorylation da kunnawa. GS-4997 yana hana samar da cytokines mai kumburi, saukar da tsarin bayyana kwayoyin halittar da ke cikin fibrosis, yana hana apoptosis mai yawa kuma yana hana yaduwar salula. |
| Saukewa: CPD100603 | Saukewa: MDK36122 | MDK36122, kuma aka sani da H-PGDS Inhibitor I, mai hana Prostaglandin D Synthase (nau'in hematopoietic). MDK36122 bashi da sunan lamba, kuma yana da CAS#1033836-12-2. An yi amfani da lambobi 5 na ƙarshe don suna don sauƙin sadarwa. MDK36122 yana toshe HPGDS (IC50s = 0.7 da 32 nM a cikin enzymes da ƙididdigar salula, bi da bi) tare da ƙaramin aiki akan enzymes ɗan adam L-PGDS, mPGES, COX-1, COX-2, da 5-LOX. |
| Saukewa: CPD100602 | Tepoxalin | Tepoxalin, wanda kuma aka sani da ORF-20485; RWJ-20485; shine mai hana 5-lipoxygenase mai yuwuwa don maganin asma, osteoarthritis (OA). Tepoxalin yana da aikin inhibitory na vivo a kan COX-1, COX-2, da 5-LOX a cikin karnuka a halin yanzu da aka yarda da shawarar da aka ba da shawarar. Tepoxalin yana haɓaka aikin antioxidant, pyrrolidine dithiocarbamate, a cikin ƙaddamar da ƙwayar cuta necrosis factor alpha-induced apoptosis a cikin ƙwayoyin WEHI 164. |
| Saukewa: CPD100601 | Tenidap | Tenidap, wanda kuma aka sani da CP-66248, mai hanawa COX / 5-LOX ne kuma dan takarar cytokine-modulating anti-inflammatory miyagun ƙwayoyi wanda Pfizer ke ci gaba da haɓakawa a matsayin mai yuwuwar jiyya ga cututtukan cututtukan rheumatoid, amma Pfizer ya dakatar da haɓakawa bayan an ƙi amincewa da tallace-tallace. da FDA a 1996 saboda hanta da koda guba, wanda aka dangana ga metabolites na miyagun ƙwayoyi tare da thiophene. kwayoyin halitta wanda ya haifar da lalacewar oxidative. |
| Saukewa: CPD100600 | Saukewa: PF-4191834 | PF-4191834 wani labari ne, mai ƙarfi da zaɓi wanda ba mai hana redox 5-lipoxygenase mai tasiri a cikin kumburi da zafi. PF-4191834 yana nuna kyakkyawan ƙarfi a cikin enzyme- da ƙididdigar tushen tantanin halitta, da kuma a cikin ƙirar bera na kumburi mai tsanani. Sakamakon bincike na Enzyme yana nuna cewa PF-4191834 shine mai hana 5-LOX mai karfi, tare da IC (50) = 229 +/- 20 nM. Bugu da ƙari kuma, ya nuna kusan 300-ninka zaɓi don 5-LOX akan 12-LOX da 15-LOX kuma ba ya nuna wani aiki ga enzymes cyclooxygenase. Bugu da ƙari, PF-4191834 yana hana 5-LOX a cikin jinin mutum, tare da IC (80) = 370 +/- 20 nM. |
| Saukewa: CPD100599 | MK-886 | MK-886, wanda kuma aka sani da L 663536, mai adawa da leukotriene. Yana iya yin wannan ta hanyar toshe furotin mai kunna 5-lipoxygenase (FLAP), don haka yana hana 5-lipoxygenase (5-LOX), kuma yana iya taimakawa wajen magance atherosclerosis. MK-886 yana hana ayyukan cyclooxygenase-1 kuma yana hana tarin platelet. MK-886 yana haifar da canje-canje a cikin sake zagayowar tantanin halitta kuma yana ƙaruwa apoptosis bayan maganin photodynamic tare da hypericin. MK-886 yana haɓaka haɓakar ƙwayar cuta necrosis factor-alpha-induced bambanci da apoptosis. |
| Saukewa: CPD100598 | L-691816 | L 691816 shine mai hanawa mai ƙarfi na amsawar 5-LO duka a cikin vitro kuma a cikin kewayon samfuran vivo. |
| Saukewa: CPD100597 | CMI-977 | CMI-977, wanda kuma aka sani da LPD-977 da MLN-977, shine mai hanawa mai 5-lipoxygenase mai ƙarfi wanda ke shiga cikin samar da leukotrienes kuma a halin yanzu ana haɓaka shi don maganin cutar asma. CMI-977 ya hana hanyar 5-lipoxygenase (5-LO) hanyar kumburin salula don toshe tsararrun leukotrienes, wanda ke taka muhimmiyar rawa wajen haifar da asma. |
| Saukewa: CPD100596 | Saukewa: CJ-13610 | CJ-13610 shine mai hanawa na baki na 5-lipoxygenase (5-LO). CJ-13610 yana hana biosynthesis na leukotriene B4 kuma yana daidaita maganganun IL-6 mRNA a cikin macrophages. Yana da tasiri a cikin preclinical model na zafi. |
| Saukewa: CPD100595 | BRP-7 | BRP-7 shine mai hana furotin mai kunnawa 5-LO (FLAP). |
| Saukewa: CPD100594 | TT15 | TT15 agonist ne na GLP-1R. |
| Saukewa: CPD100593 | Farashin 0453379 | VU0453379 shine CNS-mai shiga glucagon-kamar peptide 1 mai karɓa (GLP-1R) tabbataccen allosteric modulator (PAM) |
