| nwamba # | Aha ngwaahịa | Nkọwa |
| CPD100616 | Emricasan | Emricasan, nke a makwaara dị ka IDN 6556 na PF 03491390, bụ ihe mgbochi caspase nke mbụ na klaasị na nnwale ụlọ ọgwụ maka ọgwụgwọ ọrịa imeju. Emricasan (IDN-6556) na-ebelata mmerụ imeju na fibrosis na ụdị murine nke steatohepatitis na-abụghị mmanya. IDN6556 na-eme ka mkpirisi akuku agwaetiti dị n'akụkụ n'ime ihe nlere transplant nke agwaetiti porcine. Oral IDN-6556 nwere ike belata ọrụ aminotransferase na ndị ọrịa nwere ịba ọcha n'anya C na-adịghị ala ala. A na-ejigide PF-03491390 nke ọnụ ọnụ na imeju ruo ogologo oge na mkpughe sistemu dị ala, na-egosipụta mmetụta hepatoprotective megide mmerụ imeju nke alfa-fas na ụdị òké. . |
| CPD100615 | Q-VD-Oph | QVD-OPH, nke a makwaara dị ka Quinoline-Val-Asp-Difluorophenoxymethylketone, bụ ihe mgbochi caspase sara mbara nke nwere ikike antiapoptotic dị ike. Q-VD-OPh na-egbochi ọrịa strok nwa ọhụrụ na oke P7: ọrụ maka okike. Q-VD-OPh nwere mmetụta mgbochi ọrịa leukemia ma nwee ike ịmekọrịta na vitamin D analogs iji mee ka akara HPK1 dị na sel AML. Q-VD-OPh na-ebelata apoptosis nke na-akpata trauma ma na-eme ka mgbake nke ọrụ azụ azụ n'ime oke mgbe mmerụ ahụ gasịrị. |
| CPD100614 | Z-DEVD-FMK | Z-DEVD-fmk bụ cell-permeable, onye na-emechi ihe na-adịghị agbanwe agbanwe nke caspase-3. Caspase-3 bụ cysteinyl aspartate-kpọmkwem protease nke na-arụ ọrụ etiti na apoptosis. |
| CPD100613 | Z-IETD-FMK | MDK4982, nke a makwaara dị ka Z-IETD-FMK, bụ onye nwere ike, cell-permeable, onye na-emechi ihe na-adịghị agbanwe agbanwe nke caspase-8 na granzyme B., Caspase-8 Inhibitor II na-achịkwa ọrụ ndu nke Caspase-8. MDK4982 na-egbochi apoptosis nje butere influenza nke ọma na sel HeLa. MDK4982 na-egbochikwa granzyme B. MDK4982 nwere CAS # 210344-98-2. |
| CPD100612 | Z-VAD-FMK | Z-VAD-FMK bụ cell-permeable, onye na-egbochi pan-caspase na-apụghị ịgbagha agbagha. Z-VAD-FMK na-egbochi nhazi caspase na ntinye apoptosis na cell tumor in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 | Belnacasan | Belnacasan, nke a makwaara dị ka VX-765, ka emebere iji gbochie Caspase, nke bụ enzyme nke na-achịkwa ọgbọ nke cytokines abụọ, IL-1b na IL-18. E gosiputara VX-765 ka ọ gbochie oke ọdịdọ n'ụdị preclinical. Na mgbakwunye, VX-765 egosila ọrụ na ụdị preclinical nke Akwụkwụ na-adịghị ala ala. Ejirila VX-765 n'ime ndị ọrịa 100 n'ime oge-I na nke IIa ule ụlọ ọgwụ metụtara ọrịa ndị ọzọ, gụnyere nnwale ụlọ ọgwụ ụbọchị 28-IIa na ndị ọrịa nwere psoriasis. O mechaala usoro ọgwụgwọ nke usoro-IIa ụlọ ọgwụ nke VX-765 nke debanyere aha ihe dị ka ndị ọrịa 75 nwere akwụkwụ na-eguzogide ọgwụgwọ. Emebere nnwale ụlọ ọgwụ a na-achịkwa okpukpu abụọ, kpuru ìsì, nke a na-achịkwaghị achịkwa iji nyochaa nchekwa, nnabata na ọrụ ụlọ ọgwụ nke VX-765. |
| CPD100610 | Maraviroc | Maraviroc bụ mgbochi nje, nke nwere ike, na-enweghị asọmpi CKR-5 antagonist nke na-egbochi njikọ nke nje nje nje HIV gp120. Maraviroc na-egbochi MIP-1β-stimulated γ-S-GTP na-ejikọta na HEK-293 cell membranes, na-egosi ike ya igbochi mkpali na-adabere na chemokine nke GDP-GTP mgbanwe na CKR-5/G protein complex. Maraviroc na-egbochikwa ihe omume ala nke chemokine na-akpata redistribution calcium intracellular. |
| CPD100609 | Resatorvid | Resatorvid, nke a makwaara dị ka TAK-242, bụ onye na-egbochi cell-permeable nke TLR4, na-egbochi mmepụta LPS nke NO, TNF-α, IL-6, na IL-1β na macrophages na IC50 ụkpụrụ nke 1-11 nM. Resatorvid na-ejikọ aka na TLR4 wee gbochie mmekọrịta dị n'etiti TLR4 na ụmụ irighiri ihe nkwụnye ya. Resatorvid na-enye neuroprotection na nnwale traumatic ụbụrụ mmerụ: mmetụta na ọgwụgwọ nke ụbụrụ mmadụ |
| CPD100608 | ASK1-Inhibitor-10 | ASK1 Inhibitor 10 bụ ihe mgbochi ọnụ nke nwere ike ime ihe mgbochi apoptosis na-achịkwa kinase 1 (ASK1). Ọ bụ nhọrọ maka ASK1 karịa ASK2 yana MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, na B-RAF. Ọ na-egbochi mmụba nke streptozotocin na-ebute na JNK na p38 phosphorylation na mkpụrụ ndụ β pancreatic nke INS-1 n'ụzọ dabere na ntinye uche. |
| CPD100607 | K811 | K811 bụ ihe mgbochi ASK1 akọwapụtara nke na-agbatị ndụ n'ụdị òké nke sclerosis nke amyotrophic. K811 gbochiri nke ọma mmụba cell n'ahịrị sel nwere okwu ASK1 dị elu yana n'ime sel HER2-overexpressing GC. Ọgwụgwọ na K811 belatara nha etuto xenograft site na iwetu akara nrịbawanye. |
| CPD100606 | K812 | K812 bụ ihe mgbochi ASK1 akọwapụtara ka ọ ga-adị ogologo ndụ n'ụdị òké nke sclerosis nke amyotrophic. |
| CPD100605 | MSC-2032964A | MSC 2032964A bụ onye nwere ike na nhọrọ ASK1 inhibitor (IC50 = 93 nM). Ọ na-egbochi LPS na-ebute ASK1 na p38 phosphorylation na astrocytes òké omenala ma na-egbochi neuroinflammation na ụdị EAE òké. MSC 2032964A bụ ihe dị ndụ n'ọnụ yana ihe na-abanye n'ụbụrụ. |
| CPD100604 | Selonsertib | Selonsertib, nke a makwaara dị ka GS-4997, bụ onye na-emechi ọnụ nke ihe mgbochi nke apoptosis na-achịkwa kinase 1 (ASK1), nke nwere ike igbochi mkpali, antineoplastic na mgbochi fibrotic. GS-4997 lekwasịrị anya ma jikọta na ngalaba catalytic kinase nke ASK1 n'ụzọ asọmpi ATP, si otú a gbochie phosphorylation na ịgbalite ya. GS-4997 na-egbochi mmepụta nke cytokines na-egbuke egbuke, na-edozi okwu nke mkpụrụ ndụ ihe nketa na-etinye aka na fibrosis, na-egbochi apoptosis gabigara ókè ma gbochie mgbasawanye cellular. |
| CPD100603 | MDK36122 | MDK36122, makwaara dị ka H-PGDS Inhibitor I, bụ onye na-egbochi Prostaglandin D Synthase (ụdị hematopoietic). MDK36122 enweghị aha koodu, ma nwee CAS#1033836-12-2. Ejiri ọnụọgụ 5 ikpeazụ maka aha maka nzikọrịta ozi dị mfe. MDK36122 na-ahọrọ egbochi HPGDS (IC50s = 0.7 na 32 nM na enzyme na nyocha cellular, n'otu n'otu) na obere ọrụ megide enzymes mmadụ metụtara L-PGDS, mPGES, COX-1, COX-2, na 5-LOX. |
| CPD100602 | Tepoxalin | Tepoxalin, nke a makwaara dị ka ORF-20485; RWJ-20485; bụ 5-lipoxygenase inhibitor nwere ike maka ọgwụgwọ ụkwara ume ọkụ, osteoarthritis (OA). Tepoxalin nwere ọrụ inhibitory vivo megide COX-1, COX-2, na 5-LOX na nkịta na usoro ọgwụgwọ a kwadoro ugbu a. Tepoxalin na-akwalite ọrụ nke antioxidant, pyrrolidine dithiocarbamate, na attenuating tumor necrosis factor alpha-induced apoptosis na sel WEHI 164. |
| CPD100601 | Tenidap | Tenidap, nke a makwaara dị ka CP-66248, bụ onye na-emechi COX / 5-LOX na onye nyocha ọgwụ mgbochi cytokine-modulating nke Pfizer na-emepe emepe dị ka ọgwụgwọ na-ekwe nkwa maka ọrịa ogbu na nkwonkwo, ma Pfizer kwụsịrị mmepe mgbe a jụrụ nkwado ahịa ahịa. site na FDA na 1996 n'ihi imeju na akụrụ na-egbu egbu, nke a na-ekwu na metabolites nke ọgwụ na-eme ka ọkpụkpụ thiophene kpatara mmebi oxidative. |
| CPD100600 | PF-4191834 | PF-4191834 bụ akwụkwọ akụkọ, ike na nhọrọ na-abụghị redox 5-lipoxygenase inhibitor dị irè na mbufụt na mgbu. PF-4191834 na-egosipụta ike dị mma na nyocha enzyme- na nyocha nke cell, yana n'ụdị oke oke mbufụt. Nsonaazụ nyocha nke Enzyme na-egosi na PF-4191834 bụ ihe mgbochi 5-LOX nwere ike, yana IC (50) = 229 +/- 20 nM. Ọzọkwa, o gosipụtara ihe dịka 300-fold selectivity maka 5-LOX n'elu 12-LOX na 15-LOX ma na-egosi na ọ dịghị ọrụ na cyclooxygenase enzymes. Na mgbakwunye, PF-4191834 na-egbochi 5-LOX na sel ọbara mmadụ, yana IC (80) = 370 +/- 20 nM. |
| CPD100599 | MK-886 | MK-886, makwaara dị ka L 663536, bụ onye na-emegide leukotriene. Ọ nwere ike ime nke a site na igbochi protein 5-lipoxygenase activating (FLAP), si otú a na-egbochi 5-lipoxygenase (5-LOX), ma nwee ike inye aka n'ịgwọ atherosclerosis. MK-886 na-egbochi ọrụ cyclooxygenase-1 ma na-egbochi nchịkọta platelet. MK-886 na-ebute mgbanwe na okirikiri cell ma na-abawanye apoptosis mgbe ọgwụgwọ photodynamic na hypericin gasịrị. MK-886 na-akwalite etuto necrosis factor-alpha-induced iche na apoptosis. |
| CPD100598 | L-691816 | L 691816 bụ ihe mgbochi siri ike nke mmeghachi omume 5-LO ma in vitro na n'ọtụtụ ụdị vivo. |
| CPD100597 | CMI-977 | CMI-977, nke a makwaara dị ka LPD-977 na MLN-977, bụ ihe mgbochi 5-lipoxygenase siri ike nke na-etinye aka na mmepụta nke leukotrienes ma na-emepụta ugbu a maka ọgwụgwọ ụkwara ume ọkụ na-adịghị ala ala. CMI-977 na-egbochi ụzọ mbufụt nke 5-lipoxygenase (5-LO) iji gbochie ọgbọ nke leukotrienes, nke na-arụ ọrụ dị mkpa n'ịkpalite ụkwara ume ọkụ. |
| CPD100596 | CJ-13610 | CJ-13610 bụ onye na-egbochi ọnụ nke 5-lipoxygenase (5-LO). CJ-13610 na-egbochi biosynthesis nke leukotriene B4 ma na-achịkwa okwu IL-6 mRNA na macrophages. Ọ dị irè na ụdị mgbu mgbu. |
| CPD100595 | BRP-7 | BRP-7 bụ onye na-egbochi protein 5-LO (FLAP). |
| CPD100594 | TT15 | TT15 bụ agonist nke GLP-1R. |
| CPD100593 | VU0453379 | VU0453379 bụ CNS-penetrant glucagon-dị ka peptide 1 nnabata (GLP-1R) nti allosteric modulator (PAM) |
