| CAT # | Igama lemveliso | Inkcazo |
| CPD100567 | GW501516 | I-GW501516 yi-agonist yokwenziwa kwe-PPARδ ebonisa ukunxulumana okuphezulu kwe-PPARδ (Ki=1.1 nM) nge> 1000 yokukhetha ngaphezulu kwe-PPARα kunye ne-PPARγ. |
| CPD100566 | GFT505 | I-Elafibranor, ekwabizwa ngokuba yi-GFT-505, i-agonist ezimbini ze-PPARα/δ. I-Elafibranoris okwangoku ifundelwa unyango lwezifo ze-cardiometabolic kuquka nesifo seswekile, ukunganyangeki kwe-insulin, i-dyslipidemia, kunye nesifo se-non-alcoholic fatty (NAFLD). |
| CPD100565 | Bavachinina | I-Bavachinina yinveli yendalo ye-pan-PPAR agonist evela kwisiqhamo semveli yaseTshayina i-glucose-ukwehlisa imifuno i-malaytea scurfpea. Ibonisa imisebenzi enamandla kunye ne-PPAR-γ kune-PPAR-α kunye ne-PPAR-β / δ (EC50?=?0.74 μmol / l, 4.00 μmol / l kunye ne-8.07 μmol / l kwiiseli ze-293T, ngokulandelanayo). |
| CPD100564 | Troglitazone | I-Troglitazone, eyaziwa ngokuba yi-CI991, i-agonist enamandla ye-PPAR. I-Troglitazone i-antidiabetic kunye ne-anti-inflammatory drug, kunye nelungu leqela leziyobisi ze-thiazolidinediones. Yayimiselwe izigulana ezinesifo seswekile uhlobo lwe-2 eJapan iTroglitazone, njengezinye i-thiazolidinediones (i-pioglitazone kunye ne-rosiglitazone), isebenza ngokuvula i-peroxisome proliferator-activated receptors (PPARs). I-Troglitazone yi-ligand kuzo zombini i-PPARα kwaye - ngakumbi ngamandla - i-PPARγ |
| CPD100563 | Glabridin | I-Glabridin, enye ye-phytochemicals esebenzayo kwi-licorice extract, ibophelela kwaye isebenze i-ligand binding domain ye-PPARγ, kunye ne-receptor yobude obupheleleyo. Ikwayi-GABAA receptor positive modulator ekhuthaza i-fatty acid oxidation kunye nokuphucula ukufunda kunye nenkumbulo. |
| CPD100561 | I-Pseudoginsenoside-F11 | I-Pseudoginsenoside F11, imveliso yendalo efunyenwe kwi-ginseng yaseMelika kodwa hayi kwi-ginseng yaseAsia, yinoveli ye-PPARγ agonist yenoveli. |
| CPD100560 | Bezafibrate | I-Bezafibrate i-agonist ye-peroxisome proliferator-activated receptor alpha (PPARalpha) kunye nomsebenzi we-antilipidemic. I-Bezafibrate liyeza le-fibrate elisetyenziselwa unyango lwe-hyperlipidaemia. I-Bezafibrate yehlisa amanqanaba e-triglyceride, yonyusa amanqanaba aphezulu e-lipoprotein cholesterol, kwaye yehlise amanqanaba apheleleyo kunye asezantsi e-lipoprotein cholesterol. Idla ngokuthengiswa njengeBezalip |
| CPD100559 | GW0742 | I-GW0742, eyaziwa ngokuba yi-GW610742 kunye ne-GW0742X yi-PPARδ/β agonist. I-GW0742 yenza i-Early Neuronal Maturation ye-Cortical Post-Mitotic Neurons. I-GW0742 ikhusela i-hypertension, i-vascular inflammatory kunye nesimo se-oxidative, kunye ne-endothelial dysfunction ekutyebeni okubangelwa kukutya. I-GW0742 ineempembelelo zokukhusela ngokuthe ngqo kwi-right heart hypertrophy.GW0742 inokunyusa i-lipid metabolism entliziyweni zombini kwi-vivo kunye ne-vitro. |
| CPD100558 | I-Pioglitazone | I-Pioglitazone Hydrochloride yikhompawundi ye-thiazolidinedione echazwe ukuvelisa iziphumo ezichasayo kunye ne-antiarteriosclerotic. I-Pioglitazone iboniswa ukuthintela ukuvuvukala kwe-coronary eyenziwa yi-L-NAME kunye ne-arteriosclerosis kunye nokucinezela ukunyuka kwe-TNF-α mRNA eveliswa yi-aspirin-induced gastric mucosal injury. I-Pioglitazone Hydrochloride sisivusi se-PPAR γ |
| CPD100557 | I-Rosiglitazone | I-Rosiglitazone lichiza le-antidiabetic kudidi lwe-thiazolidinedione lwamachiza. Isebenza njenge-insulin sensitizer, ngokuzibophelela kwi-PPAR receptors kwiiseli ezinamafutha kunye nokwenza iiseli ziphendule ngakumbi kwi-insulin. I-Rosiglitazone lilungu lodidi lwe-thiazolidinedione lwamachiza. I-Thiazolidinediones isebenza njenge-insulin sensitizers. Banciphisa i-glucose, i-fatty acid, kunye ne-insulin concentrations yegazi. Basebenza ngokuzibophelela kwi-peroxisome proliferator-activated receptors (PPARs). Ii-PPAR zizinto ezibhaliweyo ezihlala kwi-nucleus kwaye zisebenze ngama-ligands afana ne-thiazolidinediones. I-Thiazolidinediones ingena kwiseli, ibophe kwii-receptors zenyukliya, kwaye iguqule ukubonakaliswa kofuzo. |
| CPD100556 | GSK0660 | I-GSK0660 ngumchasi okhethiweyo we-PPARδ. I-GSK0660 ilawulwa ngokwahlukileyo kwimibhalo ye-273 kwiiseli eziphathwe nge-TNFα xa kuthelekiswa ne-TNFα yodwa. Uhlalutyo lwendlela lubonakalise ukutyetyiswa kwe-cytokine-cytokine receptor signaling. Ngokukodwa, i-GSK0660 ivimba i-TNFα-induced upregulation ye-CCL8, i-chemokine ebandakanyekayo ekuqeshweni kwe-leukocyte. I-GSK0660 ivimba umphumo we-TNFα kwiinkcazo ze-cytokines ezibandakanyekayo ekuqeshweni kwe-leukocyte, kubandakanywa ne-CCL8, i-CCL17, kunye ne-CXCL10 kwaye ngoko ke inokuvimba i-TNFα-induced retinal leukostasis. |
| CPD100555 | Oroxin-A | I-Oroxin A, icandelo elisebenzayo elilodwa kwi-herb Oroxylum indicum (L.) Kurz, isebenze i-PPARγ kwaye inqanda i-α-glucosidase, yenza umsebenzi we-antioxidant. |
| CPD100546 | I-AZ-6102 | I-AZ6102 yi-TNKS1 / 2 inhibitor enamandla ene-100-fold selectivity ngokuchasene nezinye i-enzymes zentsapho ye-PARP kwaye ibonisa i-5 nM Wnt inhibition yendlela kwiiseli ze-DLD-1. I-AZ6102 inokuqulunqwa kakuhle kwisisombululo se-intravenous esifanelekileyo ngokweklinikhi kwi-20 mg/mL, ibonise i-pharmacokinetics efanelekileyo kwiintlobo ze-preclinical, kwaye ibonisa i-Caco2 efflux ephantsi ukuphepha iindlela zokuxhathisa ithumba. Indlela ye-canonical ye-Wnt idlala indima ebalulekileyo kuphuhliso lwe-embryonic, i-homeostasis yezicubu zabantu abadala, kunye nomhlaza. Ukuguqulwa kweGermline kumacandelo eendlela ezininzi ze-Wnt, ezifana ne-Axin, i-APC, kunye ne-?-catenin, inokukhokelela kwi-oncogenesis. Ukuvinjelwa kwe-poly(ADP-ribose) i-polymerase (PARP) i-catalytic domain ye-tankyrases (TNKS1 kunye ne-TNKS2) iyaziwa ngokunqanda indlela ye-Wnt ngokunyuka kozinzo lwe-Axin. |
| CPD100545 | KRP297 | I-KRP297, eyaziwa ngokuba yi-MK-0767 kunye ne-MK-767, i-agonist ye-PPAR enokuthi iphathe uhlobo lwe-2 yeswekile kunye ne-dyslipidemia. Xa ilawulwa kwiigundane ze-ob / ob, i-KRP-297 (i-0.3 ukuya kwi-10 mg / kg) iyancipha i-glucose ye-plasma kunye namanqanaba e-insulin kwaye yaphucula ukunyanzeliswa kwe-insulin-ivuselelwe i-2DG yokuthatha kwi-muscle ye-soleus ngendlela exhomekeke kwi-dose. Unyango lwe-KRP-297 luluncedo ekukhuseleni ukuphuhliswa kwe-syndromes yesifo sikashukela ngaphezu kokuphucula ukuthuthwa kwe-glucose ephazamisekileyo kwi-skeletal muscle. |
| CPD100543 | Inolitazone | I-Inolitazone, eyaziwa ngokuba yi-Efatutazone, i-CS-7017, kunye ne-RS5444, i-PAPR-gamma inhibitor ekhoyo ngomlomo kunye ne-antineoplastic enokubakho. I-Inolitazone ibophelela kwaye isebenze i-peroxisome proliferation-activated receptor gamma (PPAR-gamma), enokuthi ibangele ukufakwa kwe-tumor cell differentiation kunye ne-apoptosis, kunye nokunciphisa ukwanda kweseli ye-tumor. I-PPAR-gamma yi-receptor ye-hormone yenyukliya kunye ne-ligand-activated transcription factor elawula ukubonakaliswa kofuzo olubandakanyekayo kwiinkqubo zeselula ezifana nokwahlula, i-apoptosis, ulawulo lwe-cell-cycle, i-carcinogenesis, kunye nokuvutha. Khangela izilingo zeklinikhi ezisebenzayo okanye izilingo zekliniki ezivaliweyo usebenzisa le arhente. (NCI Thesaurus) |
| CPD100541 | GW6471 | I-GW6471 ngumchasi we-PPAR α (IC50 = 0.24 μ M). I-GW6471 iphucula ubudlelwane obubophezelayo be-PPAR α i-ligand-binding domain kwi-co-repressor proteins i-SMRT kunye ne-NCoR. |
| CPDD1537 | ILanifibranor | I-Lanifibranor, eyaziwa ngokuba yi-IVA-337, i-agonist ye-peroxisome proliferator-activated receptors (PPAR). |
