PPAR

CAT # Izina ryibicuruzwa Ibisobanuro
CPD100567 GW501516 GW501516 ni syntetique PPARδ yihariye agonist yerekana isano iri hejuru ya PPARδ (Ki = 1.1 nM) hamwe> guhitamo inshuro 1000 hejuru ya PPARα na PPARγ.
CPD100566 GFT505 Elafibranor, izwi kandi nka GFT-505, ni PPARα ebyiri / δ agonist. Muri iki gihe Elafibranoris iri kwigwa mu kuvura indwara z'umutima zirimo diyabete, kurwanya insuline, dyslipidemiya, n'indwara y'umwijima idafite inzoga (NAFLD).
CPD100565 Bavachinina Bavachinina ni agashya karemano-PPAR agonist kuva ku mbuto z'umuco gakondo w'Abashinwa glucose ugabanya ibyatsi malaytea scurfpea. Irerekana ibikorwa bikomeye hamwe na PPAR-γ kuruta PPAR-α na PPAR-β / δ (EC50? =? 0,74 μ mol / l, 4.00 μ mol / l na 8.07 μ mol / l muri selile 293T).
CPD100564 Troglitazone Troglitazone, izwi kandi nka CI991, ni PPAR agonist ikomeye. Troglitazone ni imiti igabanya ubukana kandi irwanya inflammatory, kandi ni umwe mu bagize ibiyobyabwenge bya thiazolidinediones. Yandikiwe abarwayi barwaye diyabete yo mu bwoko bwa 2 mu Buyapani Troglitazone, kimwe nizindi thiazolidinediones (pioglitazone na rosiglitazone), ikora mugukoresha peroxisome prolifator ikora (PPARs). Troglitazone ni ligand kuri PPARα na - cyane - PPARγ
CPD100563 Glabridin Glabridin, imwe mu mikorere ya phytochemicals ikuramo ibinyomoro, ihuza kandi igakora ligand ihuza domaine ya PPARγ, kimwe na reseptor yuzuye. Nuburyo bwa GABAA reseptor nziza modulator iteza imbere okiside ya aside irike no kunoza imyigire no kwibuka.
CPD100561 Pseudoginsenoside-F11 Pseudoginsenoside F11, ibicuruzwa bisanzwe biboneka muri ginseng yabanyamerika ariko ntabwo biri muri ginseng yo muri Aziya, ni igitabo gishya cya PPARγ agonist.
CPD100560 Bezafibrate Bezafibrate ni agoniste wa peroxisome prolifator-ikora reseptor alpha (PPARalpha) hamwe nibikorwa bya antilipidemic. Bezafibrate ni imiti ya fibrate ikoreshwa mu kuvura hyperlipidaemia. Bezafibrate igabanya urugero rwa triglyceride, ikongera urugero rwa cholesterol ya lipoprotein nyinshi, kandi ikagabanya urugero rwa cholesterol ya lipoprotein yuzuye. Bikunze kugurishwa nka Bezalip
CPD100559 GW0742 GW0742, izwi kandi nka GW610742 na GW0742X ni PPARδ / β agonist. GW0742 Itera Gukura hakiri kare ya Neuronal ya Cortical Post-Mitotic Neurons. GW0742 irinda hypertension, imiyoboro y'amaraso hamwe na okiside, hamwe no kudakora neza kwa endoteliyale mubyibushye biterwa nimirire. GW0742 igira ingaruka zitaziguye kuri hypertrophy yumutima iburyo.GW0742 irashobora kongera metabolisme ya lipide mumutima haba muri vivo ndetse no muri vitro.
CPD100558 Pioglitazone Pioglitazone Hydrochloride ni uruganda rwa thiazolidinedione rwasobanuwe kugirango rutange ingaruka za antiinflammatory na antiarteriosclerotic. Pioglitazone yerekanwa kugirango irinde L-IZINA iterwa na coronary inflammation na arteriosclerose no guhagarika TNF-α mRNA yiyongera ikorwa na aspirine iterwa no gukomeretsa mu nda. Pioglitazone Hydrochloride ni activate ya PPAR γ
CPD100557 Rosiglitazone Rosiglitazone ni imiti igabanya ubukana mu cyiciro cya thiazolidinedione. Ikora nka sensibilisateur ya insuline, muguhuza reseptor ya PPAR muma selile kandi bigatuma selile zakira insuline. Rosiglitazone numunyamuryango wa thiazolidinedione yibiyobyabwenge. Thiazolidinediones ikora nka sensibilisateur ya insuline. Bagabanya glucose, aside irike, hamwe na insuline yibanze. Bakora muguhuza peroxisome prolifator-ikora reseptors (PPARs). PPAR ni ibintu byandikirwa bibera muri nucleus hanyuma bigakorwa na ligande nka thiazolidinediones. Thiazolidinediones yinjira mu ngirabuzimafatizo, ihuza reseptor za kirimbuzi, kandi ihindura imvugo ya gen.
CPD100556 GSK0660 GSK0660 ni PPARδ yatoranijwe. GSK0660 yagenzuye mu buryo butandukanye inyandiko-mvugo 273 mu tugari twavuwe na TNFα ugereranije na TNFα yonyine. Isesengura ryinzira ryerekanaga ubutunzi bwa cytokine-cytokine reseptor signal. By'umwihariko, GSK0660 ihagarika TNFα iterwa no kugenzura CCL8, chemokine igira uruhare mu gushaka leukocyte. GSK0660 ihagarika ingaruka za TNFα ku mvugo ya cytokine igira uruhare mu kwinjiza leukocyte, harimo CCL8, CCL17, na CXCL10 bityo irashobora guhagarika TNFα iterwa na retine leukostasis.
CPD100555 Oroxin-A Oroxin A, ikintu gikora gitandukanijwe nicyatsi cya Oroxylum (L.) Kurz, ikora PPARγ kandi ikabuza α-glucosidase, ikora ibikorwa bya antioxydeant.
CPD100546 AZ-6102 AZ6102 ni inhibitor ikomeye ya TNKS1 / 2 ifite uburyo bwo guhitamo inshuro 100 kurwanya indi misemburo yumuryango wa PARP kandi ikerekana 5 nM Wnt inzira yo kubuza inzira muri selile DLD-1. AZ6102 irashobora gutegurwa neza mugisubizo kijyanye na clinique yumuti winjiza kuri mg / mL 20, yerekanye imiti ya farumasi nziza mumoko yabanjirije, kandi yerekana Caco2 efflux nkeya kugirango hirindwe uburyo bwo kurwanya ibibyimba bishoboka. Inzira ya Canonical Wnt igira uruhare runini mugukuza urusoro, ingirabuzimafatizo zikuze homeostasis, na kanseri. Imiterere ya Germline yibice byinshi byinzira ya Wnt, nka Axin, APC, na? -Catenin, irashobora gutera oncogenez. Kubuza poly (ADP-ribose) polymerase (PARP) catalitike ya tankiras (TNKS1 na TNKS2) izwiho guhagarika inzira ya Wnt binyuze mukwiyongera kwa Axin.
CPD100545 KRP297 KRP297, izwi kandi nka MK-0767 na MK-767, ni PPAR agonist ishobora kuvura diyabete yo mu bwoko bwa 2 na dyslipidemiya. Iyo ikozwe ku mbeba za ob / ob, KRP-297 (0.3 kugeza 10 mg / kg) yagabanije plasma glucose na insuline kandi inonosora insuline iterwa na insuline iterwa na 2DG mu mitsi ya soleus muburyo buterwa na dose. Ubuvuzi bwa KRP-297 ni ingirakamaro mu gukumira indwara ya syndromes ya diyabete usibye no kunoza ubwikorezi bwa glucose bwangiritse mu mitsi ya skeletale.
CPD100543 Inolitazone Inolitazone, izwi kandi nka Efatutazone, CS-7017, na RS5444, ni bioavailable yo mu kanwa PAPR-gamma inhibitor ifite ibikorwa bya antineoplastique. Inolitazone ihuza kandi igakora peroxisome ikwirakwizwa na reseptor gamma (PPAR-gamma), ishobora kuvamo kwinjiza uturemangingo twibibyimba na apoptose, ndetse no kugabanuka kwikwirakwizwa rya selile. PPAR-gamma ni reseptor ya hormone ya nucleaire hamwe na ligand ikoreshwa na transcription transcription igenzura imvugo ya gene igira uruhare mubikorwa bya selile nko gutandukanya, apoptose, kugenzura ingirabuzimafatizo, kanseri, no gutwika. Reba ibizamini bya clinique ikora cyangwa ibizamini bya clinique bifunze ukoresheje iyi agent. (NCI Thesaurus)
CPD100541 GW6471 GW6471 ni PPAR α antagonist (IC50 = 0.24 μ M). GW6471 yongerera imbaraga guhuza PPAR α ligand-binding domaine hamwe na poroteyine ya co-repressor SMRT na NCoR.
CPDD1537 Lanifibranor Lanifibranor, izwi kandi nka IVA-337, ni peroxisome prolifator-ikora reseptor (PPAR) agonist.
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