| CAT # | Product Name | Tsanangudzo |
| CPD100616 | Emricasan | Emricasan, inozivikanwawo seIDN 6556 uye PF 03491390, ndiyo yekutanga-in-class caspase inhibitor mumakiriniki ekuedzwa kwekurapa kwezvirwere zvechiropa. Emricasan (IDN-6556) inoderedza kukuvara kwechiropa uye fibrosis mumurine modhi yeasiri doro steatohepatitis. IDN6556 inogonesa marginal mass islet engraftment mune porcine islet autotransplant modhi. Oral IDN-6556 inogona kuderedza basa reaminotransferase kune varwere vane chirwere chisingaperi chehepatitis C. Inoshandiswa nemuromo-PF-03491390 inochengetwa muchiropa kwenguva yakareba ine yakaderera systemic exposure, ichiita hepatoprotective effect kurwisa alpha-fas-induced chiropa kukuvara mumuenzaniso wembeva. . |
| CPD100615 | Q-VD-Oph | QVD-OPH, inozivikanwawo seQuinoline-Val-Asp-Difluorophenoxymethylketone, yakafara spectrum caspase inhibitor ine simba antiapoptotic properties. Q-VD-OPh inodzivirira neonatal sitiroko muP7 rat: basa revakadzi. Q-VD-OPh ine anti-leukemia mhedzisiro uye inogona kudyidzana nevhitamini D analogs kuwedzera HPK1 kusaina mumaseru AML. Q-VD-OPh inoderedza kushungurudzika-induced apoptosis uye inovandudza kudzoreredza kwemashure-enhengo basa mumakonzo mushure mekukuvara kwemusana. |
| CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk is cell-permeable, irreversible inhibitor ye caspase-3. Caspase-3 inonzi cysteineyl aspartate-specific protease inoita basa guru muapoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, inozivikanwawo seZ-IETD-FMK, ine simba, cell-permeable, irreversible inhibitor ye caspase-8 uye granzyme B., The Caspase-8 Inhibitor II inodzora biological chiitiko cheCaspase-8. MDK4982 inonyatso inhibits influenza virus-induced apoptosis mumasero eHeLa. MDK4982 zvakare inhibits granzyme B. MDK4982 ine CAS#210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK is cell-permeable, irreversible pan-caspase inhibitor. Z-VAD-FMK inhibits caspase processing uye apoptosis induction mu tumor cell in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, inozivikanwawo seVX-765, yakagadzirirwa kuvharidzira Caspase, iri enzyme inodzora chizvarwa chema cytokines maviri, IL-1b uye IL-18. VX-765 yakaratidzwa kuti inhibit acute seizures mu preclinical modhi. Uye zvakare, VX-765 yakaratidza chiitiko mu preclinical modhi yechirwere chepfari. VX-765 yakanga yaiswa muvarwere vanopfuura 100 muchikamu-I uye chikamu-IIa miedzo yemakiriniki ine chokuita nezvimwe zvirwere, kusanganisira 28-day phase-IIa kliniki yekuedza kune varwere vane psoriasis. Yakapedza chikamu chekurapa chechikamu-IIa kliniki yekuedza yeVX-765 iyo yakanyora vangangoita 75 varwere vane kurapa-inodzivirira pfari. Iyo yakapetwa kaviri-mapofu, randomized, placebo-inodzorwa kliniki yekuedza yakagadzirirwa kuongorora kuchengeteka, kushivirira uye kliniki chiitiko cheVX-765. |
| CPD100610 | Maraviroc | Maraviroc inorwisa mavhairasi, ine simba, isina kukwikwidza CKR-5 receptor antagonist inodzivisa kusunga kweHIV viral coat protein gp120. Maraviroc inhibits MIP-1β-inosimudzira γ-S-GTP inosunga kuHEK-293 cell membranes, ichiratidza kukwanisa kwayo kudzivisa chemokine-inotsamira kukurudzira kweGDP-GTP kuchinjana paCKR-5/G protein complex. Maraviroc inodzivisawo chiitiko chepasi che chemokine-induced intracellular calcium redistribution. |
| CPD100609 | Resatorvid | Resatorvid, inozivikanwawo seTAK-242, inonzi cell-permeable inhibitor yeTLR4 chiratidzo, ichivharira LPS-induced production yeNO, TNF-α, IL-6, uye IL-1β mumacrophages ane IC50 maitiro e1-11 nM. Resatorvid inosunga yakasarudzika kuTLR4 uye inovhiringa kudyidzana pakati peTLR4 nemamorekuru ayo eadapter. Resatorvid inopa neuroprotection mukuyedza kushungurudza kukuvara kwehuropi: zvinoreva mukurapwa kwekukuvara kwehuropi hwemunhu |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 is an olly bioavailable inhibitor yeapoptosis signal-regulating kinase 1 (ASK1). Inosarudza ASK1 pamusoro peASK2 uyewo MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, uye B-RAF. Inodzivisa kuwedzera kwe streptozotocin-induced muJNK uye p38 phosphorylation mu INS-1 pancreatic β masero muhutano-hunoenderana. |
| CPD100607 | K811 | K811 inonzi ASK1-specific inhibitor inorebesa kurarama mumhando yembeva yeamyotrophic lateral sclerosis. K811 yakanyatso dzivirira kupararira kwesero mumitsetse yemasero ane yakakwira ASK1 kutaura uye muHER2-overexpressing GC masero. Kurapa neK811 kwakaderedzwa hukuru hwemamota exenograft nekudzikisira mamaki ekuwedzera. |
| CPD100606 | K812 | K812 inonzi ASK1-specific inhibitor yakawanikwa kuti irebese kurarama mumhando yembeva yeamyotrophic lateral sclerosis. |
| CPD100605 | MSC-2032964A | MSC 2032964A ine simba uye inosarudza ASK1 inhibitor (IC50 = 93 nM). Iyo inovhara LPS-induced ASK1 uye p38 phosphorylation mune yakasimwa mbeva astrocytes uye inodzvanya neuroinflammation mune mbeva EAE modhi. MSC 2032964A inowanikwa nemuromo uye inopinda muuropi. |
| CPD100604 | Selonsertib | Selonsertib, inozivikanwawo se GS-4997, inonzi orally bioavailable inhibitor yeapoptosis signal-regulating kinase 1 (ASK1), ine zvinogona anti-inflammatory, antineoplastic uye anti-fibrotic zviitiko. GS-4997 inotarisa uye inosungira kune catalytic kinase domain ye ASK1 nenzira yeATP-yemakwikwi, nokudaro ichidzivirira phosphorylation uye activation. GS-4997 inodzivirira kugadzirwa kweanopisa cytokines, pasi-inogadzirisa kutaura kwemajini anobatanidzwa mufibrosis, inodzvinyirira yakawandisa apoptosis uye inhibits kupararira kwesero. |
| CPD100603 | MDK36122 | MDK36122, inozivikanwawo seH-PGDS Inhibitor I, iProstaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 haina kodhi zita, uye ine CAS#1033836-12-2. Yekupedzisira 5-manhamba yakashandiswa pazita rekutaura kuri nyore. MDK36122 inovhara HPGDS (IC50s = 0.7 uye 32 nM mune enzyme uye cellular assays, zvichiteerana) nekuita kushoma kunopesana nema enzymes evanhu L-PGDS, mPGES, COX-1, COX-2, uye 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, inozivikanwawo seORF-20485; RWJ-20485; inonzi 5-lipoxygenase inhibitor inogona kurapa asthma, osteoarthritis (OA). Tepoxalin ine mu vivo inhibitory basa rinopesana neCOX-1, COX-2, uye 5-LOX mumbwa pane ikozvino yakagamuchirwa inokurudzirwa dosage.Tepoxalin inhibits kuzvimba uye microvascular dysfunction inokonzerwa neabdominal irradiation mumakonzo. Tepoxalin inowedzera basa re antioxidant, pyrrolidine dithiocarbamate, mukuderedza tumor necrosis factor alpha-induced apoptosis muWEHI 164 masero. |
| CPD100601 | Tenidap | Tenidap, inozivikanwawo seCP-66248, ndeye COX/5-LOX inhibitor uye cytokine-modulating anti-inflammatory drug candidate yakanga iri pasi pekuvandudzwa naPfizer seanovimbisa kurapa rheumatoid arthritis, asi Pfizer akamisa budiriro mushure mekunge mvumo yekushambadzira yarambwa. neFDA muna 1996 nekuda kwechiropa uye chepfu yeitsvo, iyo yainzi yakakonzerwa nematabolites e mushonga une thiophene moiety iyo yakakonzera oxidative kukuvara. |
| CPD100600 | PF-4191834 | PF-4191834 ibhuku, rine simba uye rinosarudza risina redox 5-lipoxygenase inhibitor inoshanda mukuzvimba uye kurwadziwa. PF-4191834 inoratidza yakanaka potency mune enzyme- uye maseru-based assays, pamwe neiyo rat modhi yekuzvimba kwakanyanya. Enzyme assay mhedzisiro inoratidza kuti PF-4191834 ine simba 5-LOX inhibitor, ine IC(50) = 229 +/- 20 nM. Uyezve, yakaratidza inenge 300-fold selectivity ye5-LOX pamusoro pe12-LOX uye 15-LOX uye hairatidzi basa kune cyclooxygenase enzymes. Mukuwedzera, PF-4191834 inhibits 5-LOX mumasero eropa evanhu, ine IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, inozivikanwawo seL 663536, inopikisa leukotriene. Inogona kuita izvi nekuvhara 5-lipoxygenase activating protein (FLAP), nokudaro inhibiting 5-lipoxygenase (5-LOX), uye inogona kubatsira mukurapa atherosclerosis. MK-886 inhibits cyclooxygenase-1 basa uye inodzvinyirira platelet aggregation. MK-886 induces shanduko mu cell cycle uye inowedzera apoptosis mushure me photodynamic therapy ne hypericin. MK-886 inowedzera tumor necrosis factor-alpha-induced differentiation uye apoptosis. |
| CPD100598 | L-691816 | L 691816 inhibitor ine simba yeiyo 5-LO maitiro ese ari mu vitro uye mune akasiyana emhando dze vivo. |
| CPD100597 | CMI-977 | CMI-977, inozivikanwawo seLPD-977 uye MLN-977, ine simba 5-lipoxygenase inhibitor inopindira mukugadzirwa kweleukotrienes uye parizvino iri kugadzirwa kuti irapwe asthma isingaperi. CMI-977 inhibits iyo 5-lipoxygenase (5-LO) masero ekuputira nzira yekuvhara chizvarwa che leukotrienes, iyo inoita basa rinokosha mukukonzera bronchial asthma. |
| CPD100596 | CJ-13610 | CJ-13610 inonzi orally active inhibitor ye5-lipoxygenase (5-LO) . CJ-13610 inhibits biosynthesis ye leukotriene B4 uye inogadzirisa IL-6 mRNA kutaura mu macrophages. Inoshanda mune preclinical mhando dzemarwadzo. |
| CPD100595 | BRP-7 | BRP-7 ndeye 5-LO activating protein (FLAP) inhibitor. |
| CPD100594 | TT15 | TT15 inyanzvi yeGLP-1R. |
| CPD100593 | VU0453379 | VU0453379 ndeye CNS-inopinda glucagon-yakaita peptide 1 receptor (GLP-1R) yakanaka allosteric modulator (PAM) |
