| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100567 | GW501516 | I-GW501516 iyi-agonist yokwenziwa ye-PPARδ ebonisa ukuhlobana okuphezulu kwe-PPARδ (Ki=1.1 nM) ngokukhetha okugoqiwe okungu-1000 ngaphezu kwe-PPARα ne-PPARγ. |
| I-CPD100566 | GFT505 | I-Elafibranor, eyaziwa nangokuthi i-GFT-505, iyi-agonist ekabili ye-PPARα/δ. I-Elafibranoris okwamanje ifundelwa ukwelashwa kwezifo ze-cardiometabolic kuhlanganise nesifo sikashukela, ukumelana ne-insulin, i-dyslipidemia, nesifo sesibindi esinamafutha angenalo utshwala (NAFLD). |
| I-CPD100565 | Bavachina | I-Bavachinina iyinoveli ye-pan-PPAR agonist yemvelo evela esithelweni sekhambi lendabuko laseShayina elehlisa i-glucose i-malaytea scurfpea. Ibonisa imisebenzi enamandla nge-PPAR-γ kune-PPAR-α ne-PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l kanye no-8.07 μmol/l kumaseli angu-293T, ngokulandelana). |
| I-CPD100564 | I-Troglitazone | I-Troglitazone, eyaziwa nangokuthi i-CI991, iyi-agonist enamandla ye-PPAR. I-Troglitazone iyisidakamizwa esilwa nokuvuvukala kanye ne-antidiabetic, futhi iyilungu lesigaba sezidakamizwa se-thiazolidinediones. Yayimiselwe iziguli ezinesifo sikashukela sohlobo 2 eJapan i-Troglitazone, njengezinye i-thiazolidinediones (i-pioglitazone ne-rosiglitazone), isebenza ngokwenza kusebenze i-peroxisome proliferator-activated receptors (PPARs). I-Troglitazone iyi-ligand yakho kokubili i-PPARα futhi - kakhulu - i-PPARγ |
| I-CPD100563 | I-Glabridin | I-Glabridin, enye ye-phytochemicals esebenzayo ekukhishweni kwe-licorice, ibophezela futhi isebenze isizinda sokubopha i-ligand se-PPARγ, kanye ne-receptor yobude obugcwele. Iphinde ibe i-GABAA receptor positive modulator ekhuthaza i-fatty acid oxidation futhi ithuthukise ukufunda nenkumbulo. |
| I-CPD100561 | I-Pseudoginsenoside-F11 | I-Pseudoginsenoside F11, umkhiqizo wemvelo otholakala ku-ginseng yaseMelika kodwa hhayi ku-ginseng yase-Asia, iyinoveli eyingxenye ye-PPARγ agonist. |
| I-CPD100560 | I-Bezafibrate | I-Bezafibrate iyi-agonist ye-peroxisome proliferator-activated receptor alpha (PPARalpha) enomsebenzi we-antilipidemic. I-Bezafibrate iyisidakamizwa se-fibrate esisetshenziselwa ukwelapha i-hyperlipidemia. I-Bezafibrate yehlisa amazinga e-triglyceride, ikhuphule amazinga aphezulu we-lipoprotein cholesterol, futhi yehlise inani eliphelele neliphansi lama-lipoprotein cholesterol. Ivame ukudayiswa njenge-Bezalip |
| I-CPD100559 | GW0742 | I-GW0742, eyaziwa nangokuthi i-GW610742 kanye ne-GW0742X i-agonist ye-PPARδ/β. I-GW0742 Idala Ukuvuthwa Kwangaphambi KweNeuronal Kwe-Cortical Post-Mitotic Neurons. I-GW0742 ivimbela umfutho wegazi ophakeme, isimo se-vascular inflammatory kanye ne-oxidative, kanye nokungasebenzi kwe-endothelial ekukhuluphaleni okubangelwa ukudla. I-GW0742 inemiphumela yokuvikela eqondile ku-hypertrophy yenhliziyo engakwesokudla.I-GW0742 ingase ithuthukise i-lipid metabolism enhliziyweni kokubili ku-vivo kanye ne-vitro. |
| I-CPD100558 | I-Pioglitazone | I-Pioglitazone Hydrochloride iyinhlanganisela ye-thiazolidinedione echazwa ukukhiqiza imiphumela elwa nokuvuvukala kanye ne-antiarteriosclerotic. I-Pioglitazone iboniswa ukuvimbela ukuvuvukala kwe-coronary okubangelwa i-L-NAME kanye ne-arteriosclerosis kanye nokucindezela ukwanda kwe-TNF-α mRNA ekhiqizwa i-aspirin-induced gastric mucosal mucosal. I-Pioglitazone Hydrochloride iyi-activator ye-PPAR γ |
| I-CPD100557 | I-Rosiglitazone | I-Rosiglitazone iyisidakamizwa se-antidiabetic esekilasini lezidakamizwa ze-thiazolidinedione. Isebenza njengesensitizer ye-insulin, ngokubopha kuma-receptors e-PPAR kumaseli amafutha nokwenza amangqamuzana aphendule kakhudlwana ku-insulin. I-Rosiglitazone iyilungu leqembu lezidakamizwa ze-thiazolidinedione. I-Thiazolidinediones isebenza njenge-insulin sensitizer. Banciphisa i-glucose, i-fatty acid, kanye nokugxila kwe-insulin egazini. Asebenza ngokubopha kuma-peroxisome proliferator-activated receptors (PPARs). Ama-PPAR yizici zokuloba ezihlala ku-nucleus futhi zenziwa zisebenze ama-ligand afana ne-thiazolidinediones. I-Thiazolidinediones ingena kuseli, ibopha kuma-nuclear receptors, futhi iguqule ukubonakaliswa kwezakhi zofuzo. |
| I-CPD100556 | I-GSK0660 | I-GSK0660 iyimbangi ye-PPARδ ekhethiwe. I-GSK0660 ilawule ngokuhlukile imibhalo engu-273 kumaseli aphathwe nge-TNFα uma kuqhathaniswa ne-TNFα kuphela. Ukuhlaziywa kwendlela yembula ukunothiswa kokusayina kwe-cytokine-cytokine receptor. Ikakhulukazi, i-GSK0660 ivimba ukukhushulwa kwe-TNFα-induced ye-CCL8, i-chemokine ehilelekile ekubuthweni kwe-leukocyte. I-GSK0660 ivimbela umphumela we-TNFα emazwini ama-cytokines ahilelekile ekubuthweni kwe-leukocyte, okuhlanganisa i-CCL8, i-CCL17, ne-CXCL10 ngakho-ke ingase ivimbele i-leukostasis ye-retinal eyenziwe yi-TNFα. |
| I-CPD100555 | I-Oroxin-A | I-Oroxin A, isakhi esisebenzayo esihlukanisiwe nekhambi i-Oroxylum indicum (L.) Kurz, yenza kusebenze i-PPARγ futhi ivimbele i-α-glucosidase, yenza umsebenzi wokulwa ne-antioxidant. |
| I-CPD100546 | I-AZ-6102 | I-AZ6102 iyisivimbeli esinamandla se-TNKS1/2 esinokukhetha okuphindwe izikhathi ezingu-100 ngokumelene namanye ama-enzyme omndeni we-PARP futhi ebonisa ukuvinjelwa kwendlela engu-5 nM Wnt kumaseli e-DLD-1. I-AZ6102 ingenziwa kahle esisombululo esifanelekile somtholampilo esingu-20 mg/mL, ibonise i-pharmacokinetics ezinhle ezinhlotsheni zangaphambi komtholampilo, futhi ikhombisa ukwehla kwe-Caco2 efflux ukugwema izindlela ezingase zibe khona zokumelana nesimila. Indlela ye-Wnt ye-canonical idlala indima ebalulekile ekukhuleni kwe-embryonic, i-homeostasis yezicubu zabantu abadala, kanye nomdlavuza. Ukuguqulwa kwe-germline kwezingxenye ezimbalwa zendlela ye-Wnt, njenge-Axin, i-APC, ne-?-catenin, kungaholela ku-oncogenesis. Ukuvinjelwa kwesizinda se-poly(ADP-ribose) polymerase (PARP) se-tankyrases (TNKS1 kanye ne-TNKS2) kwaziwa ngokuvimbela indlela ye-Wnt ngokunyusa ukuzinza kwe-Axin. |
| I-CPD100545 | I-KRP297 | I-KRP297, eyaziwa nangokuthi i-MK-0767 kanye ne-MK-767, iyi-agonist ye-PPAR okungenzeka yokwelapha uhlobo lwesifo sikashukela sohlobo 2 kanye ne-dyslipidemia. Lapho isetshenziswa kumagundane e-ob/ob, i-KRP-297 (0.3 kuya ku-10 mg/kg) yehlisa i-plasma glucose kanye namazinga e-insulin futhi yathuthukisa ukutholwa kwe-2DG ekhiqizwe i-insulin engasebenzi kahle emcupheni owodwa ngendlela encike kumthamo. Ukwelashwa kwe-KRP-297 kuyasiza ukuvimbela ukuthuthukiswa kwesifo sikashukela ngaphezu kokunciphisa ukuthuthwa kwe-glucose ephazamisekile emisipha yamathambo. |
| I-CPD100543 | Inolitazone | I-Inolitazone, eyaziwa nangokuthi i-Efatutazone, CS-7017, kanye ne-RS5444, iyisivimbeli esitholakala ngomlomo se-PAPR-gamma esinamandla okwenza umsebenzi we-antineoplastic. I-Inolitazone ibophezela futhi yenze kusebenze i-peroxisome proliferation-activated receptor gamma (PPAR-gamma), okungase kuphumele ekuqalisweni kokuhlukaniswa kweseli yesimila kanye ne-apoptosis, kanye nokwehliswa kokwanda kweseli yesimila. I-PPAR-gamma iyisamukeli sehomoni yenuzi kanye nesici sokuloba esicushwe yi-ligand esilawula ukuvezwa kofuzo okubandakanyeka ezinqubweni zamaselula njengokuhlukanisa, i-apoptosis, ukulawula umjikelezo wamaseli, i-carcinogenesis, nokuvuvukala. Hlola izivivinyo zomtholampilo ezisebenzayo noma izivivinyo zomtholampilo ezivaliwe usebenzisa lesi sisebenzeli. (NCI Thesaurus) |
| I-CPD100541 | GW6471 | I-GW6471 iyimbangi ye-PPAR α (IC50 = 0.24 μ M). I-GW6471 ithuthukisa ukuhambisana okubophezelayo kwesizinda esibophezelayo se-PPAR α kumaprotheni e-co-repressor SMRT kanye ne-NCoR. |
| I-CPDD1537 | I-Lanifibranor | I-Lanifibranor, eyaziwa nangokuthi i-IVA-337, iyi-agonist ye-peroxisome proliferator-activated receptors (PPAR). |
