| CAT # | Khoom npe | Kev piav qhia |
| PAB 100567 | wb 501516 | GW501516 yog ib qho hluavtaws PPARδ-specific agonist uas qhia cov affinity siab rau PPARδ (Ki = 1.1 nM) nrog> 1000 fold selectivity tshaj PPARα thiab PPARγ. |
| PIB 100566 | GFT505 | Elafibranor, tseem hu ua GFT-505, yog dual PPARα / δ agonist. Elafibranoris tam sim no tau kawm los kho cov kab mob cardiometabolic nrog rau ntshav qab zib, insulin tsis kam, dyslipidemia, thiab kab mob tsis muaj dej cawv fatty siab (NAFLD). |
| PIB 100565 | Bavachinina | Bavachinina yog ib qho tshiab ntuj yias-PPAR agonist los ntawm cov txiv hmab txiv ntoo ntawm cov tsoos suav qab zib-txo tshuaj ntsuab malaytea scurfpea. Nws qhia tau hais tias muaj zog ua haujlwm nrog PPAR-γ dua li nrog PPAR-α thiab PPAR-β / δ (EC50? = 0.74 μmol / l, 4.00 μmol / l thiab 8.07 μmol / l hauv 293T hlwb, ntsig txog). |
| PIB 100564 | Troglitazone | Troglitazone, tseem hu ua CI991, yog tus muaj zog PPAR agonist. Troglitazone yog ib qho tshuaj tiv thaiv kab mob ntshav qab zib thiab tshuaj tiv thaiv kab mob, thiab cov tswv cuab ntawm pawg tshuaj ntawm thiazolidinediones. Nws tau raug sau tseg rau cov neeg mob ntshav qab zib hom 2 hauv Nyij Pooj Troglitazone, zoo li lwm yam thiazolidinediones (pioglitazone thiab rosiglitazone), ua haujlwm los ntawm kev ua kom muaj zog peroxisome proliferator-activated receptors (PPARs). Troglitazone yog ligand rau PPARα thiab - ntau zog - PPARγ |
| PIB 100563 | Glabridin | Glabridin, ib qho ntawm cov phytochemicals nquag hauv licorice extract, khi rau thiab ua kom lub ligand binding domain ntawm PPARγ, nrog rau tag nrho ntev receptor. Nws kuj yog GABAA receptor zoo modulator txhawb fatty acid oxidation thiab txhim kho kev kawm thiab nco. |
| PIB 100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, ib yam khoom ntuj pom nyob rau hauv American ginseng tab sis tsis nyob rau hauv Asian ginseng, yog ib feem tshiab PPARγ agonist. |
| PIB 100560 | Bezafibrate | Bezafibrate yog ib qho agonist ntawm peroxisome proliferator-activated receptor alpha (PPARalpha) nrog cov tshuaj tiv thaiv kab mob. Bezafibrate yog ib qho tshuaj fiber ntau siv rau kev kho mob hyperlipidemia. Bezafibate txo cov roj lipoprotein ntau ntau li cov roj cholesterol, thiab cov roj cholesterol tsawg. Nws yog feem ntau ua lag luam li Bezalip |
| PIB 100559 | wb 0742 | GW0742, tseem hu ua GW610742 thiab GW0742X yog PPARδ/β agonist. GW0742 Induces Early Neuronal Maturation ntawm Cortical Post-Mitotic Neurons. GW0742 tiv thaiv kev kub siab, vascular inflammatory thiab oxidative xwm txheej, thiab endothelial tsis ua hauj lwm nyob rau hauv kev noj haus vim rog. GW0742 muaj kev tiv thaiv ncaj qha rau ntawm txoj cai lub plawv hypertrophy.GW0742 tuaj yeem txhim kho lipid metabolism hauv plawv ob leeg hauv vivo thiab hauv vitro. |
| PIB 100558 | Pioglitazone | Pioglitazone Hydrochloride yog ib qho thiazolidinedione compound uas tau piav qhia los tsim cov tshuaj tiv thaiv kab mob thiab cov tshuaj tiv thaiv arteriosclerotic. Pioglitazone tau pom los tiv thaiv L-NAME-induced coronary o thiab arteriosclerosis thiab inhibit TNF-α mRNA uas ua los ntawm cov tshuaj aspirin-induced gastric mucosal raug mob. Pioglitazone Hydrochloride yog ib qho activator ntawm PPAR γ |
| PIB 100557 | Rosiglitazone | Rosiglitazone yog cov tshuaj tiv thaiv kab mob ntshav qab zib hauv cov tshuaj thiazolidinedione. Nws ua haujlwm raws li cov tshuaj insulin, los ntawm kev khi rau PPAR receptors hauv cov rog rog thiab ua rau lub hlwb ua haujlwm ntau dua rau insulin. Rosiglitazone yog ib tug tswv cuab ntawm thiazolidinedione chav kawm ntawm cov tshuaj. Thiazolidinediones ua raws li cov tshuaj insulin. Lawv txo cov piam thaj, fatty acids, thiab insulin hauv cov ntshav. Lawv ua haujlwm los ntawm kev khi rau peroxisome proliferator-activated receptors (PPARs). PPARs yog cov kev hloov pauv uas nyob hauv lub nucleus thiab ua haujlwm los ntawm ligands xws li thiazolidinediones. Thiazolidinediones nkag mus rau hauv lub cell, khi rau cov receptors nuclear, thiab hloov cov kev qhia ntawm cov noob. |
| PIB 100556 | KWS 0660 | GSK0660 yog xaiv PPARδ antagonist. GSK0660 sib txawv tswj 273 cov ntawv teev lus hauv TNFα-kho hlwb piv rau TNFα ib leeg. Ib txoj hauv kev tsom xam tau qhia txog kev txhim kho ntawm cytokine-cytokine receptor signaling. Tshwj xeeb, GSK0660 blocks TNFα-induced upregulation ntawm CCL8, ib tug chemokine koom nrog hauv kev nrhiav neeg ua haujlwm leukocyte. GSK0660 thaiv cov nyhuv ntawm TNFα ntawm cov lus qhia ntawm cytokines koom nrog hauv kev nrhiav neeg ua haujlwm leukocyte, suav nrog CCL8, CCL17, thiab CXCL10 thiab nws tuaj yeem thaiv TNFα-induced retinal leukostasis. |
| PIB 100555 | Oroxin-A | Oroxin A, ib qho active tivthaiv cais los ntawm cov tshuaj ntsuab Oroxylum indicum (L.) Kurz, activates PPARγ thiab inhibits α-glucosidase, exerting antioxidant kev ua si. |
| PIB 100546 | Qauv: AZ-6102 | AZ6102 yog ib qho muaj zog TNKS1/2 inhibitor uas muaj 100-fold selectivity tiv thaiv lwm cov PARP tsev neeg enzymes thiab qhia 5 nM Wnt txoj kev inhibition hauv DLD-1 hlwb. AZ6102 tuaj yeem tsim tau zoo nyob rau hauv kev kho mob cov tshuaj intravenously ntawm 20 mg / mL, tau pom zoo pharmacokinetics nyob rau hauv preclinical hom, thiab qhia tau hais tias tsawg Caco2 efflux kom tsis txhob muaj cov qog ua hauj lwm mechanisms. Txoj kev canonical Wnt plays lub luag haujlwm tseem ceeb hauv kev loj hlob ntawm embryonic, cov neeg laus cov ntaub so ntswg homeostasis, thiab mob qog noj ntshav. Germline kev hloov pauv ntawm ntau yam Wnt txoj hauv kev, xws li Axin, APC, thiab ?-catenin, tuaj yeem ua rau oncogenesis. Inhibition ntawm poly (ADP-ribose) polymerase (PARP) catalytic domain ntawm lub tankyrases (TNKS1 thiab TNKS2) paub tias inhibit Wnt txoj hauv kev los ntawm kev nce stabilization ntawm Axin. |
| PIB 100545 | PAB 297 | KRP297, tseem hu ua MK-0767 thiab MK-767, yog PPAR agonist uas muaj peev xwm kho mob ntshav qab zib hom 2 thiab dyslipidemia. Thaum muab tshuaj rau ob / ob nas, KRP-297 (0.3 mus rau 10 mg / kg) txo cov ntshav qabzib hauv cov ntshav thiab cov tshuaj insulin thiab txhim kho qhov tsis zoo ntawm cov tshuaj insulin-stimulated 2DG uptake hauv cov leeg nqaij nyob rau hauv ib koob tshuaj. Kev kho KRP-297 yog qhov tseem ceeb los tiv thaiv kev txhim kho ntawm cov mob ntshav qab zib mellitus ntxiv rau kev ua kom lub cev tsis muaj zog ntawm cov piam thaj hauv cov leeg pob txha. |
| PIB 100543 | Inolitazone | Inolitazone, tseem hu ua Efatutazone, CS-7017, thiab RS5444, yog ib qho bioavailable PAPR-gamma inhibitor uas muaj peev xwm ua haujlwm antineoplastic. Inolitazone khi rau thiab ua kom peroxisome proliferation-activated receptor gamma (PPAR-gamma), uas yuav ua rau induction ntawm qog cell txawv thiab apoptosis, nrog rau txo cov qog cell proliferation. PPAR-gamma yog ib qho tshuaj hormone receptor thiab ligand-activated transcription yam tswj cov noob qhia koom nrog hauv cov txheej txheem ntawm tes xws li kev sib txawv, apoptosis, kev tswj lub voj voog ntawm tes, carcinogenesis, thiab o. Tshawb xyuas cov kev sim tshuaj kho mob lossis kaw qhov kev sim tshuaj uas siv tus neeg sawv cev no. (NCI Thesaurus) |
| PIB 100541 | wb 6471 | GW6471 yog PPAR α antagonist (IC50 = 0.24 μ M). GW6471 txhim kho qhov kev sib txuas ntawm PPAR α ligand-binding domain rau cov co-repressor proteins SMRT thiab NCoR. |
| TIAB SA 1537 | Lanifibranor | Lanifibranor, tseem hu ua IVA-337, yog peroxisome proliferator-activated receptors (PPAR) agonist. |
