CAT # | Magaca Alaabta | Sharaxaada |
CPD100567 | GW501516 | GW501516 waa agonist gaar ah oo PPARδ-synthetic ah oo muujisa xidhiidh sare oo loogu talagalay PPARδ (Ki=1.1 nM) oo leh> 1000 laab xulashada PPARA iyo PPARγ. |
CPD100566 | GFT505 | Elafibranor, oo sidoo kale loo yaqaan GFT-505, waa laba-geesoodka PPARA/δ. Elafibranoris hadda waxaa lagu bartaa daaweynta cudurada wadnaha oo ay ku jiraan sonkorowga, caabbinta insulin, dyslipidemia, iyo cudurka beerka dufanka aan khamriga ahayn (NAFLD). |
CPD100565 | Bavachinina | Bavachinina waa sheeko dabiici ah oo dabiici ah PPAR agonist oo ka timid midhaha geedaha gulukooska hoos u dhiga Shiinaha ee scurfpea. Waxay muujinaysaa waxqabadyo ka xoog badan PPAR-γ marka loo eego PPAR-α iyo PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l iyo 8.07 μmol/l ee unugyada 293T, siday u kala horreeyaan). |
CPD100564 | Troglitazone | Troglitazone, oo sidoo kale loo yaqaan CI991, waa agonist PPAR awood leh. Troglitazone waa daawada ka hortagga sonkorowga iyo ka hortagga bararka, iyo xubin ka mid ah fasalka daroogada ee thiazolidinediones. Waxaa loo qoray bukaanada qaba sonkorowga mellitus nooca 2 ee Japan Troglitazone, sida thiazolidinediones kale (pioglitazone iyo rosiglitazone), waxay u shaqeysaa iyada oo kicinaysa soo-dhoweynta proliferator-activated peroxisome (PPARs). Troglitazone waa isku xidhka labada PPARA iyo – aad uga xoog badan – PPARγ |
CPD100563 | Glabridin | Glabridin, mid ka mid ah phytochemicals firfircoon ee laga soosaaray licorice, waxay ku xidhaa oo ay dhaqaajisaa qaybta xidhitaanka ligand ee PPARγ, iyo sidoo kale dhererka dhererka buuxa. Sidoo kale waa GABAA receptor togan modulator kor u qaada oksaydhka dufanka leh iyo hagaajinta barashada iyo xusuusta. |
CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, oo ah badeecad dabiici ah oo laga helo ginseng American laakiin aan ku jirin ginseng Asian, waa qayb cusub oo PPARγ agonist ah. |
CPD100560 | Bezafibrate | Bezafibrate waa agonist of peroxisome proliferator-activated receptor alpha (PPARalpha) oo leh firfircooni antilipidemie ah. Bezafibrate waa daawo fibrate ah oo loo isticmaalo daawaynta hyperlipidemia. Bezafibrate waxay hoos u dhigtaa heerarka triglyceride, waxay kordhisaa cufnaanta sare ee lipoprotein kolestaroolka, waxayna hoos u dhigtaa wadarta iyo cufnaanta hoose ee heerarka kolestaroolka. Waxaa caadi ahaan loo suuq geeyaa sida Bezalip |
CPD100559 | GW0742 | GW0742, sidoo kale loo yaqaan GW610742 iyo GW0742X waa PPARδ/β agonist. GW0742 Waxay keentaa korriinka neerfaha hore ee neerfayaasha-mitotic-ka ee kortikal. GW0742 waxay ka hortagtaa hypertension, bararka xididada xididada iyo heerka oksaydhiyaha, iyo cillad la'aanta endothelial ee buurnaanta cuntada ay keentay. GW0742 waxay leedahay saameyn difaac toos ah oo ku saabsan hypertrophy wadnaha saxda ah. |
CPD100558 | Pioglitazone | Pioglitazone Hydrochloride waa iskudhis thiazolidinedione lagu tilmaamay inay soo saarto saamaynta anti-bararka iyo antiarteriosclerotic. Pioglitazone waxaa loo soo bandhigay si looga hortago caabuqa wadnaha ee L-NAME-ku keeno iyo arteriosclerosis iyo in la xakameeyo kororka TNF-α mRNA ee ay soo saarto asbiriin-ku-saare xuubka caloosha. Pioglitazone Hydrochloride waa firfircooni PPAR γ |
CPD100557 | Rosiglitazone | Rosiglitazone waa daawada ka hortagga sonkorowga ee fasalka thiazolidinedione ee daawooyinka. Waxay u shaqeysaa sidii dareenka insulin-ta, iyadoo ku xiraysa soo-dhoweeyayaasha PPAR ee unugyada baruurta iyo samaynta unugyadu kuwo aad uga jawaaba insulinta. Rosiglitazone waa xubin ka mid ah daawada thiazolidinedione. Thiazolidinediones waxay u shaqeeyaan sidii dareenka insulin-ta. Waxay yareeyaan gulukooska, aashitada dufanka leh, iyo uruurinta dhiiga insulinta. Waxay ku shaqeeyaan iyagoo ku xiraya soo-dhoweeyayaasha proliferator-activated peroxisome (PPARs). PPARs waa arrimo qoraal ah oo ku nool xudunta waxayna noqdaan kuwo firfircoon oo isku xiran sida thiazolidinediones. Thiazolidinediones waxay galaan unugga, waxay ku xidhaan reseptors nukliyeerka, waxayna beddelaan muujinta hiddo-wadaha. |
CPD100556 | GSK0660 | GSK0660 waa PPARδ antagonist door ah. GSK0660 ayaa si kala duwan u habeeyey 273 qoraallada ku jira unugyada TNFa-daaweeyay marka la barbar dhigo TNFa oo keliya. Falanqaynta dariiqa ayaa shaaca ka qaaday kobcinta calaamadaha cytokine-cytokine reseptor. Gaar ahaan, GSK0660 waxay xannibaysaa kor u qaadista TNFa-ku-abuurtay ee CCL8, kiimiko ku lug leh qoritaanka leukocyte. GSK0660 waxay xannibaysaa saamaynta TNFa ee tibaaxaha cytokines ee ku lug leh qoritaanka leukocyte, oo ay ku jiraan CCL8, CCL17, iyo CXCL10 oo sidaas awgeed waxay xannibi kartaa TNFa-ku-soo-baxa leukostasis retinal. |
CPD100555 | Oroxin-A | Oroxin A, oo ah qayb firfircoon oo ka go'an geedaha Oroxylum indicum (L.) Kurz, waxay kicisaa PPARγ waxayna joojisaa α-glucosidase, oo qabata dhaqdhaqaaqa antioxidant. |
CPD100546 | AZ-6102 | AZ6102 waa TNKS1/2 horjooge awood leh oo leh 100-laab xulashada enzymes kale ee qoyska PARP oo muujiya xannibaadda 5 nM Wnt ee unugyada DLD-1. AZ6102 si fiican ayaa loo qaabayn karaa xalal xididada ku habboon kiliinikada ee 20 mg / mL, waxay muujisay farmashiyaha wanaagsan ee noocyada preclinical, waxayna muujinaysaa hooseeya Caco2 efflux si looga fogaado hababka iska caabbinta buro ee suurtogalka ah. Waddada canonical Wnt waxay door muhiim ah ka ciyaartaa korriinka uurjiifka, homeostasis unugga dadka waaweyn, iyo kansarka. Isbeddellada jeermiska ee dhowr qaybood oo Wnt ah, sida Axin, APC, iyo ?-catenin, waxay u horseedi kartaa kansarka. Joojinta poly (ADP-ribose) polymerase (PARP) catalytic domain ee tankyrases (TNKS1 iyo TNKS2) ayaa loo yaqaanaa inay joojiyaan dariiqa Wnt iyada oo loo marayo xasilinta kordhinta Axin. |
CPD100545 | KRP297 | KRP297, oo sidoo kale loo yaqaan MK-0767 iyo MK-767, waa PPAR agonist awood u leh daaweynta nooca 2 ee sonkorowga iyo dyslipidemia. Marka la maamulo jiirarka ob/ob, KRP-297 (0.3 ilaa 10 mg/kg) waxay hoos u dhigtay gulukooska balaasmaha iyo heerarka insulinta waxayna wanaajisay insulin-kicinta 2DG ee daciifka ah ee muruqa soleus qaab ku tiirsan qiyaasta. Daaweynta KRP-297 ayaa faa'iido leh si looga hortago horumarinta cilladaha sonkorowga marka lagu daro hagaajinta gaadiidka gulukooska ee daciifka ah ee muruqa lafaha. |
CPD100543 | Inolitazone | Inolitazone, oo sidoo kale loo yaqaan Efatutazone, CS-7017, iyo RS5444, waa inhibitor PAPR-gamma afka laga heli karo oo leh firfircoonida antineoplastic. Inolitazone waxay ku xidhan tahay oo ay kicisaa peroxisome proliferation-activated receptor gamma (PPAR-gamma), taas oo laga yaabo inay keento soo-saarka kala-duwanaanta unugyada burooyinka iyo apoptosis, iyo sidoo kale hoos u dhigista kororka unugyada burooyinka. PPAR-gamma waa soo-dhoweeyaha hoormoonka nukliyeerka iyo ligand-activated transcription factor oo xakameynaya muujinta hidda-socodka ee ku lug leh hababka gacanta sida kala-duwanaanta, apoptosis, xakamaynta wareegga unugyada, kansarka, iyo bararka. Hubi tijaabooyin caafimaad oo firfircoon ama tijaabooyin caafimaad oo xidhan adoo isticmaalaya wakiilkan. (NCI Thesaurus) |
CPD100541 | GW6471 | GW6471 waa PPAR α antagonist (IC50 = 0.24 μM). GW6471 waxay wanaajisaa isku xidhka xidhidhiyaha PPAR α ligand-ku xidhidhiyaha borotiinada isku xidhka SMRT iyo NCoR. |
CPDD1537 | Lanifibranor | Lanifibranor, oo sidoo kale loo yaqaan IVA-337, waa daaweeyayaasha proliferator-activated peroxisome (PPAR) agonist. |