| MPAKA # | Dzina lazogulitsa | Kufotokozera |
| CPD100567 | GW501516 | GW501516 ndi agonist wopangidwa ndi PPARδ yemwe amawonetsa kuyanjana kwakukulu kwa PPARδ (Ki=1.1 nM) ndi> kusankha kwa 1000 mopitilira PPARα ndi PPARγ. |
| CPD100566 | GFT505 | Elafibranor, yemwe amadziwikanso kuti GFT-505, ndi wapawiri PPARα/δ agonist. Elafibranoris pakali pano akuphunziridwa pofuna kuchiza matenda a cardiometabolic kuphatikizapo matenda a shuga, insulin resistance, dyslipidemia, ndi matenda osamwa mowa mwauchidakwa (NAFLD). |
| Chithunzi cha CPD100565 | Bavachinina | Bavachinina ndi buku lachilengedwe la pan-PPAR agonist kuchokera ku chipatso cha chikhalidwe cha China chotsitsa shuga malaytea scurfpea. Zimasonyeza ntchito zamphamvu ndi PPAR-γ kusiyana ndi PPAR-α ndi PPAR-β / δ (EC50?=?0.74 μmol / l, 4.00 μmol / l ndi 8.07 μmol / l mu maselo a 293T, motsatira). |
| Mtengo wa CPD100564 | Troglitazone | Troglitazone, yemwenso amadziwika kuti CI991, ndi wamphamvu PPAR agonist. Troglitazone ndi antidiabetic komanso anti-yotupa mankhwala, ndi membala wa gulu la mankhwala a thiazolidinediones. Adalangizidwa kwa odwala omwe ali ndi matenda a shuga amtundu wa 2 ku Japan Troglitazone, monga thiazolidinediones (pioglitazone ndi rosiglitazone), amagwira ntchito poyambitsa ma receptor a peroxisome proliferator-activated (PPARs). Troglitazone ndi ligand kwa onse PPARα ndipo - mwamphamvu kwambiri - PPARγ |
| CPD100563 | Glabridin | Glabridin, imodzi mwazinthu zogwira ntchito za phytochemicals mu chotsitsa cha licorice, zimamangiriza ndikuyambitsa chigawo chomangirira cha ligand cha PPARγ, komanso cholandirira chonse. Ilinso ndi GABAA receptor positive modulator yolimbikitsa mafuta acid oxidation ndikuwongolera kuphunzira ndi kukumbukira. |
| CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, chinthu chachilengedwe chopezeka mu ginseng waku America koma osati mu ginseng waku Asia, ndi buku la PPARγ agonist. |
| CPD100560 | Bezafibrate | Bezafibrate ndi agonist wa peroxisome proliferator-activated receptor alpha (PPARalpha) ndi antilipidemic zochita. Bezafibrate ndi mankhwala a fibrate omwe amagwiritsidwa ntchito pochiza hyperlipidemia. Bezafibrate imachepetsa milingo ya triglyceride, imachulukitsa kuchuluka kwa lipoprotein cholesterol, ndikuchepetsa kuchuluka kwamafuta amafuta a lipoprotein otsika komanso otsika. Amagulitsidwa kwambiri ngati Bezalip |
| CPD100559 | GW0742 | GW0742, yomwe imadziwikanso kuti GW610742 ndi GW0742X ndi PPARδ/β agonist. GW0742 Imapangitsa Kukula Kwambiri Kwa Neuronal kwa Cortical Post-Mitotic Neurons. GW0742 imalepheretsa kuthamanga kwa magazi, kutupa kwa mitsempha ndi oxidative, ndi endothelial dysfunction mu zakudya zomwe zimayambitsa kunenepa kwambiri. GW0742 ili ndi zotsatira zotetezera mwachindunji pa hypertrophy ya mtima wamanja.GW0742 ikhoza kupititsa patsogolo kagayidwe ka lipid mu mtima mu vivo ndi mu vitro. |
| CPD100558 | Pioglitazone | Pioglitazone Hydrochloride ndi gulu la thiazolidinedione lomwe limafotokozedwa kuti limatulutsa anti-inflammatory and antiarteriosclerotic effect. Pioglitazone imawonetseredwa kuti imalepheretsa kutupa kwa mtima kwa L-NAME ndi arteriosclerosis komanso kupondereza kuchuluka kwa TNF-α mRNA yopangidwa ndi aspirin-induced gastric mucosal kuvulala. Pioglitazone Hydrochloride ndi activator wa PPAR γ |
| CPD100557 | Rosiglitazone | Rosiglitazone ndi mankhwala oletsa shuga m'gulu la thiazolidinedione. Imagwira ntchito ngati chodziwikiratu cha insulin, pomanga ma receptor a PPAR m'maselo amafuta ndikupanga ma cell kulabadira insulin. Rosiglitazone ndi membala wa gulu la thiazolidinedione. Thiazolidinediones amagwira ntchito ngati zolimbikitsa insulin. Amachepetsa shuga, mafuta acid, komanso kuchuluka kwa insulin m'magazi. Amagwira ntchito pomanga ku peroxisome proliferator-activated receptors (PPARs). Ma PPAR ndi zinthu zolembera zomwe zimakhala mumphuno ndipo zimayendetsedwa ndi ma ligand monga thiazolidinediones. Thiazolidinediones amalowa m'selo, amamangiriza ku zolandilira za nyukiliya, ndikusintha mawonekedwe a majini. |
| CPD100556 | GSK0660 | GSK0660 ndi mdani wosankha wa PPARδ. GSK0660 imawongolera mosiyanasiyana zolemba za 273 m'maselo othandizidwa ndi TNFα poyerekeza ndi TNFα yokha. Kusanthula kwa njira kunawonetsa kulemerera kwa cytokine-cytokine receptor signing. Makamaka, GSK0660 imalepheretsa kuwongolera kwa TNFα kwa CCL8, chemokine yomwe imagwira ntchito polemba leukocyte. GSK0660 imalepheretsa zotsatira za TNFα pamawu a ma cytokines omwe amakhudzidwa ndi kulembedwa kwa leukocyte, kuphatikizapo CCL8, CCL17, ndi CXCL10 ndipo chifukwa chake akhoza kulepheretsa TNFα-induced retinal leukostasis. |
| CPD100555 | Oroxin-A | Oroxin A, chigawo chogwira ntchito chodzipatula ku therere Oroxylum indicum (L.) Kurz, imayendetsa PPARγ ndikuletsa α-glucosidase, kuchita ntchito ya antioxidant. |
| CPD100546 | AZ-6102 | AZ6102 ndi inhibitor yamphamvu ya TNKS1 / 2 yomwe ili ndi kusankha kwa 100 motsutsana ndi ma enzyme ena a banja la PARP ndipo imasonyeza 5 nM Wnt njira yolepheretsa m'maselo a DLD-1. AZ6102 imatha kupangidwa bwino mu njira yolumikizira mtsempha ya 20 mg/mL, yawonetsa ma pharmacokinetics abwino m'mitundu yodziwika bwino, ndipo ikuwonetsa kutsika kwa Caco2 efflux kupeŵa njira zomwe zingatheke kukana chotupa. Njira yovomerezeka ya Wnt imagwira ntchito yofunika kwambiri pakukula kwa embryonic, homeostasis yamagulu akuluakulu, komanso khansa. Kusintha kwa majeremusi kwa zigawo zingapo za njira ya Wnt, monga Axin, APC, ndi ?-catenin, kungayambitse ku oncogenesis. Kuletsa kwa poly(ADP-ribose) polymerase (PARP) chothandizira dera la tankyrases (TNKS1 ndi TNKS2) amadziwika kuti amalepheretsa njira ya Wnt kudzera pakuwonjezereka kwa Axin. |
| CPD100545 | KRP297 | KRP297, yomwe imadziwikanso kuti MK-0767 ndi MK-767, ndi PPAR agonist yemwe angathe kuchiza matenda a shuga a mtundu wa 2 ndi dyslipidemia. Pogwiritsidwa ntchito ku mbewa za ob/ob, KRP-297 (0.3 mpaka 10 mg/kg) inachepetsa kuchuluka kwa shuga m'magazi a plasma ndi insulini ndikuwongolera kutengeka kwa 2DG kwa insulin m'minofu yokhayokha motengera mlingo. Chithandizo cha KRP-297 ndi chothandiza poletsa kukula kwa matenda a shuga kuphatikiza pakuwongolera kusokonezeka kwa kayendedwe ka shuga m'chigoba. |
| CPD100543 | Inolitazone | Inolitazone, yomwe imadziwikanso kuti Efatutazone, CS-7017, ndi RS5444, ndi inhibitor yapakamwa ya PAPR-gamma yomwe imatha kuchitapo kanthu. Inolitazone imamangiriza ndikuyambitsa peroxisome proliferation-activated receptor gamma (PPAR-gamma), zomwe zingapangitse kupangidwa kwa chotupa kusiyanitsa ndi apoptosis, komanso kuchepetsa kuchuluka kwa maselo a chotupa. PPAR-gamma ndi cholandilira cha nyukiliya cha nyukiliya ndi ligand-activated transcript factor yomwe imayang'anira mawonekedwe a jini omwe amakhudzidwa ndi ma cell monga kusiyanitsa, apoptosis, cell-cycle control, carcinogenesis, ndi kutupa. Yang'anani mayesero azachipatala omwe akugwira ntchito kapena mayesero otsekedwa achipatala pogwiritsa ntchito wothandizira uyu. (NCI Thesaurus) |
| CPD100541 | GW6471 | GW6471 ndi PPAR α wotsutsa (IC50 = 0.24 μ M). GW6471 imakulitsa mgwirizano womangirira wa PPAR α ligand-binding domain ku mapuloteni a co-repressor SMRT ndi NCoR. |
| Chithunzi cha CPDD1537 | Lanifibranor | Lanifibranor, yemwenso amadziwika kuti IVA-337, ndi peroxisome proliferator-activated receptors (PPAR) agonist. |
