| PUSI # | Igoa Oloa | Fa'amatalaga |
| CPD100567 | GW501516 | GW501516 o se agonist faʻapitoa PPARδ faʻapitoa e faʻaalia ai le maualuga o le vavalalata mo PPARδ (Ki = 1.1 nM) faʻatasi ai ma> 1000 fold selectivity i luga ole PPARα ma PPARγ. |
| CPD100566 | GFT505 | Elafibranor, e lauiloa foi o le GFT-505, o se PPARα / δ agonist lua. Elafibranoris o loʻo suʻesuʻeina nei mo le togafitia o faʻamaʻi cardiometabolic e aofia ai le maʻisuka, insulin resistance, dyslipidemia, ma le faʻamaʻi gaʻo gaʻo ole ava (NAFLD). |
| CPD100565 | Bavachinina | O le Bavachinina ose fa'ama'i fa'alenatura pan-PPAR mai le fua o le la'au fa'a-Saina e fa'aitiitia ai le kulukose malaytea scurfpea. O loʻo faʻaalia ai le malosi o gaioiga faʻatasi ma le PPAR-γ nai lo le PPAR-α ma le PPAR-β / δ (EC50? =? 0.74 μmol / l, 4.00 μmol / l ma le 8.07 μmol / l i 293T sela, faasologa). |
| CPD100564 | Troglitazone | Troglitazone, e taʻua foi o le CI991, o se vailaʻau malosi PPAR. Troglitazone o se vailaʻau faʻamaʻi ma anti-inflammatory, ma o se sui o le vasega o vailaʻau o le thiazolidinediones. Na faʻatonuina mo tagata mamaʻi e maua i le maʻisuka ituaiga 2 i Iapani Troglitazone, pei o isi thiazolidinediones (pioglitazone ma rosiglitazone), e galue e ala i le faʻagaoioia o le peroxisome proliferator-activated receptors (PPARs). Troglitazone o se ligand i le PPARα ma - sili atu le malosi - PPARγ |
| CPD100563 | Glabridin | Glabridin, o se tasi o vailaʻau faʻamalosi malosi i le licorice extract, e fusifusia ma faʻagaoioia le ligand binding domain o le PPARγ, faʻapea foʻi ma le umi o le tali. O le GABAA fo'i le fa'aogaina lelei o le modulator e fa'aolaina ai le ga'o ga'o fa'ama'i ma fa'aleleia le a'oa'oina ma le manatua. |
| CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, ose oloa fa'anatura o lo'o maua i le ginseng Amerika ae le o le ginseng Asia, o se tala fa'apitoa PPARγ agonist. |
| CPD100560 | Bezafibrate | Bezafibrate o se agonist o le peroxisome proliferator-activated receptor alpha (PPARalpha) faʻatasi ai ma gaioiga antilipidemic. Bezafibrate o se vailaʻau fibrate faʻaaogaina mo togafitiga o le hyperlipidemia. O le Bezafibrate e fa'aitiitia ai le maualuga o le triglyceride, fa'ateleina le maualuga o le lipoprotein cholesterol, ma fa'aitiitia le aofa'i ma le maualalo o le lipoprotein cholesterol maualuga. E masani ona maketiina e pei o Bezalip |
| CPD100559 | GW0742 | GW0742, faʻaigoaina GW610742 ma GW0742X o se PPARδ/β agonist. GW0742 Faʻaosoina le vave faʻatupuina o le Neuronal o Cortical Post-Mitotic Neurons. GW0742 puipuia le toto maualuga, vascular inflammatory ma oxidative tulaga, ma le endothelial dysfunction i meaʻai-faʻaosoina obesity. GW0742 e iai a'afiaga puipuia sa'o ile hypertrophy o le fatu taumatau.GW0742 e mafai ona fa'aleleia ai le lipid metabolism i le fatu i vivo ma in vitro. |
| CPD100558 | Pioglitazone | O le Pioglitazone Hydrochloride o se thiazolidinedione tu'ufa'atasi o lo'o fa'amatalaina e maua ai a'afiaga fa'ama'i ma fa'ama'i. O le Pioglitazone o lo'o fa'aalia e puipuia ai le afaina o le fatu ma le arteriosclerosis L-NAME ma taofia ai le fa'ateleina o le TNF-α mRNA na gaosia e le aspirin-fa'aosoina manu'a mucosal gastric. Pioglitazone Hydrochloride o se fa'agaioiga ole PPAR γ |
| CPD100557 | Rosiglitazone | Rosiglitazone o se vailaʻau antidiabetic i le vasega thiazolidinedione o vailaʻau. E galue e pei o se inisalini sensitizer, e ala i le fusifusia i le PPAR receptors i sela gaʻo ma faʻafaigofie ai sela i le inisalini. Rosiglitazone o se sui o le thiazolidinedione vasega o vailaʻau. Thiazolidinediones e galue e pei o le insulin sensitizers. Latou te fa'aitiitia le kulukose, ga'o ga'o, ma le inisalini toto. Latou te galulue e ala i le fusifusia i le peroxisome proliferator-activated receptors (PPARs). PPARs o mea faʻaliliuga o loʻo nofo i totonu o le nucleus ma faʻagaoioia e ligands pei o thiazolidinediones. Thiazolidinediones ulu atu i totonu o le sela, fusifusia i le faaniukilia talipupuni, ma suia le faʻaaliga o kenera. |
| CPD100556 | GSK0660 | GSK0660 o se fili filifilia PPARδ antagonist. GSK0660 faʻatulafonoina faʻatulafonoina 273 transcripts i sela TNFα-togafitiga faʻatusatusa ile TNFα naʻo. O se suʻesuʻega auala na faʻaalia ai le faʻatamaoaigaina o le faʻailoga o le faʻailoga o le cytokine-cytokine. Aemaise lava, GSK0660 poloka le TNFα-induced upregulation o le CCL8, o se chemokine o loʻo aʻafia i le leukocyte recruitment. GSK0660 poloka le aʻafiaga o le TNFα i luga o faʻamatalaga o cytokines o loʻo aʻafia i le leukocyte recruitment, e aofia ai le CCL8, CCL17, ma le CXCL10 ma e ono poloka ai le TNFα-induced retinal leukostasis. |
| CPD100555 | Oroxin-A | Oroxin A, o se vaega malosi e vavae ese mai le vao Oroxylum indicum (L.) Kurz, faʻagaoioia PPARγ ma faʻalavelaveina le α-glucosidase, faʻaaogaina gaioiga antioxidant. |
| CPD100546 | AZ-6102 | AZ6102 o se TNKS1 / 2 inhibitor malosi lea e 100-filifili filifili e faasaga i isi enzymes aiga PARP ma faʻaalia 5 nM Wnt ala faʻalavelave i sela DLD-1. O le AZ6102 e mafai ona faʻatulagaina lelei i totonu ole vailaʻau faʻamaʻi talafeagai ile 20 mg / mL, ua faʻaalia lelei pharmacokinetics i ituaiga preclinical, ma faʻaalia le maualalo o le Caco2 efflux e aloese ai mai faʻaogaina o le tumo. E taua tele le sao ole auala Wnt ile tuputupu a'e ole pepe, homeostasis a tagata matutua, ma le kanesa. O suiga ole Germline o nisi o vaega ole ala Wnt, e pei ole Axin, APC, ma le ?-catenin, e mafai ona o'o atu ai ile oncogenesis. O le taofiofia o le poly (ADP-ribose) polymerase (PARP) catalytic domain o tankyrases (TNKS1 ma TNKS2) ua iloa e taofia ai le ala Wnt e ala i le faʻaleleia atili o le Axin. |
| CPD100545 | KRP297 | KRP297, e lauiloa foi o MK-0767 ma MK-767, o se PPAR agonist e mafai mo togafitiga o le maʻisuka ituaiga 2 ma le dyslipidemia. Pe a tuʻuina atu i isumu ob / ob, KRP-297 (0.3 i le 10 mg / kg) faʻaititia le kulukose plasma ma le inisalini maualuga ma faʻaleleia le faʻaleagaina o le inisalini-stimulated 2DG uptake i musele soleus i se fua faʻalagolago. KRP-297 togafitiga e aoga e puipuia ai le atinaʻeina o faʻamaʻi maʻisuka faʻaopoopo i le faʻaleleia o le faʻaleagaina o le kulukose felauaiga i maso skeletal. |
| CPD100543 | Inolitazone | Inolitazone, e ta'ua fo'i o Efatutazone, CS-7017, ma le RS5444, ose fa'ato'aga PAPR-gamma e mafai ona tu'u gutu ma e mafai ona fa'agaioia antineoplastic. O le Inolitazone e fusifusia ma faʻagaoioia le peroxisome proliferation-activated receptor gamma (PPAR-gamma), lea e ono iʻu ai i le faʻaosoina o le eseesega o le tumo ma le apoptosis, faʻapea foʻi ma le faʻaitiitia o le faʻateleina o le tumo. O le PPAR-gamma o se faʻaogaina o le homone faaniukilia ma le ligand-activated transcription factor e pulea ai le faʻaaliga o kenera e aʻafia i ia faʻagasologa feaveaʻi e pei o le eseesega, apoptosis, pulea o le taamilosaga, carcinogenesis, ma le mumū. Siaki mo faʻataʻitaʻiga faʻapitoa faʻataʻitaʻiga poʻo faʻataʻitaʻiga tapuni faʻataʻitaʻiga e faʻaaoga ai lenei sooupu. (NCI Thesaurus) |
| CPD100541 | GW6471 | GW6471 o le PPAR α antagonist (IC50 = 0.24 μ M). GW6471 faʻaleleia le fesoʻotaʻiga vavalalata o le PPAR α ligand-binding domain i le co-repressor proteins SMRT ma NCoR. |
| CPDD1537 | Lanifibranor | Lanifibranor, lea e taʻua foi o le IVA-337, o le peroxisome proliferator-activated receptors (PPAR) agonist. |
