| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100567 | GW501516 | GW501516 ke agonist ea maiketsetso ea PPARδ-specific e bonts'ang kamano e phahameng bakeng sa PPARδ (Ki=1.1 nM) ka > khetho e 1000 ho feta PPARα le PPARγ. |
| CPD100566 | GFT505 | Elafibranor, eo hape e tsejoang e le GFT-505, ke agonist e habeli ea PPARα/δ. Elafibranoris hajoale e ntse e ithutoa bakeng sa kalafo ea mafu a pelo a kenyelletsang lefu la tsoekere, insulin resistance, dyslipidemia, le lefu la sebete le se nang joala le mafura (NAFLD). |
| CPD100565 | Bavachina | Bavachinina ke pale ea tlhaho ea pan-PPAR agonist e tsoang litholoana tsa setlama sa setso sa China se theolang tsoekere ea malaytea scurfpea. E bontša mesebetsi e matla ka PPAR-γ ho feta ka PPAR-α le PPAR-β / δ (EC50?=?0.74 μmol / l, 4.00 μmol / l le 8.07 μmol / l ka lisele tsa 293T, ka ho latellana). |
| CPD100564 | Troglitazone | Troglitazone, eo hape e tsejoang e le CI991, ke agonist e matla ea PPAR. Troglitazone ke sethethefatsi se thibelang lefu la tsoekere le se khahlanong le ho ruruha, hape ke setho sa sehlopha sa lithethefatsi sa thiazolidinediones. E ne e laetsoe bakuli ba nang le lefu la tsoekere la mofuta oa 2 ba Japane Troglitazone, joalo ka thiazolidinediones tse ling (pioglitazone le rosiglitazone), e sebetsa ka ho kenya tšebetsong li-receptor tsa peroxisome proliferator-activated (PPARs). Troglitazone ke ligand ho PPARα ka bobeli le - ka matla le ho feta - PPARγ |
| CPD100563 | Glabridin | Glabridin, e 'ngoe ea li-phytochemicals tse sebetsang ka har'a licorice extract, e tlama le ho kenya tšebetsong sebaka se tlamang sa ligand sa PPARγ, hammoho le receptor ea bolelele bo felletseng. Hape ke GABAA receptor positive modulator e khothalletsang mafura a acid oxidation le ho ntlafatsa ho ithuta le mohopolo. |
| CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, sehlahisoa sa tlhaho se fumanehang ho ginseng ea Amerika empa eseng ho ginseng ea Asia, ke agonist ea karolo ea PPARγ. |
| CPD100560 | Bezafibrate | Bezafibrate ke agonist ea peroxisome proliferator-activated receptor alpha (PPARalpha) e nang le ts'ebetso ea antilipidemic. Bezafibrate ke setlhare sa fibrate se sebelisetsoang ho phekola hyperlipidemia. Bezafibrate e fokotsa maemo a triglyceride, e eketsa maemo a k'holeseterole e phahameng ea density lipoprotein, 'me e theole boemo ba k'holeseterole e felletseng le e tlase. Hangata e rekisoa e le Bezalip |
| CPD100559 | GW0742 | GW0742, e tsejoang hape e le GW610742 le GW0742X ke PPARδ/β agonist. GW0742 E Etsa Hore ho be le Phallo ea Pele ea Neuronal ea Cortical Post-Mitotic Neurons. GW0742 e thibela khatello ea mali, boemo ba vascular inflammatory le oxidative, le ho se sebetse ha endothelial ka botenya bo bakoang ke lijo. GW0742 e na le liphello tse tobileng tse sireletsang ho hypertrophy ea pelo e nepahetseng.GW0742 e ka ntlafatsa metabolism ea lipid ka pelong ka bobeli ka vivo le in vitro. |
| CPD100558 | Pioglitazone | Pioglitazone Hydrochloride ke motsoako oa thiazolidinedione o hlalosoang ho hlahisa litlamorao tse thibelang ho ruruha le antiarteriosclerotic. Pioglitazone e bontšoa ho thibela ho ruruha ha pelo e bakoang ke L-NAME le arteriosclerosis le ho hatella ho eketseha ha TNF-α mRNA e hlahisoang ke aspirin-induced gastric mucosal kotsi. Pioglitazone Hydrochloride ke activator ea PPAR γ |
| CPD100557 | Rosiglitazone | Rosiglitazone ke sethethefatsi sa antidiabetic sa sehlopha sa thiazolidinedione. E sebetsa joalo ka sensitizer ea insulin, ka ho tlama li-receptor tsa PPAR liseleng tsa mafura le ho etsa hore lisele li arabele insulin haholoanyane. Rosiglitazone ke setho sa sehlopha sa thiazolidinedione. Thiazolidinediones e sebetsa e le li-sensitizers tsa insulin. Ba fokotsa tsoekere, acid e mafura le insulin maling. Li sebetsa ka ho tlama ho li-receptors tsa peroxisome proliferator-activated (PPARs). Li-PPAR ke lintlha tse ngotsoeng tse lulang khubung 'me li sebelisoa ke li-ligand tse kang thiazolidinediones. Li-thiazolidinediones li kena ka seleng, li tlama ho li-receptor tsa nyutlelie, 'me li fetola ponahalo ea liphatsa tsa lefutso. |
| CPD100556 | GSK0660 | GSK0660 ke mohanyetsi ea khethang oa PPARδ. GSK0660 e laola ka tsela e fapaneng litlaleho tsa 273 liseleng tse tšoaroang ke TNFα ha li bapisoa le TNFα feela. Tlhahlobo ea litsela e senotse ntlafatso ea pontšo ea cytokine-cytokine receptor. Ka ho khetheha, GSK0660 e thibela TNFα-induced upregulation ea CCL8, chemokine e amehang ho hira leukocyte. GSK0660 e thibela phello ea TNFα holim'a lipolelo tsa li-cytokine tse amehang mosebetsing oa ho hira leukocyte, ho akarelletsa le CCL8, CCL17, le CXCL10 'me ka hona e ka thibela TNFα-induced retinal leukostasis. |
| CPD100555 | Oroxin-A | Oroxin A, karolo e sebetsang e arohaneng le setlama sa Oroxylum indicum (L.) Kurz, e kenya tshebetsong PPARγ mme e thibela α-glucosidase, e fana ka ts'ebetso ea antioxidant. |
| CPD100546 | AZ-6102 | AZ6102 ke inhibitor e matla ea TNKS1 / 2 e nang le khetho ea makhetlo a 100 khahlanong le li-enzyme tse ling tsa lelapa la PARP 'me e bontša ho thibela tsela ea 5 nM Wnt liseleng tsa DLD-1. AZ6102 e ka etsoa hantle ka tharollo ea methapo e amanang le kliniki ho 20 mg/mL, e bonts'itse pharmacokinetics e ntle mefuteng ea preclinical, mme e bonts'a matla a tlase a Caco2 ho qoba mekhoa e ka bang teng ea ho hanyetsa hlahala. Tsela ea canonical Wnt e phetha karolo ea bohlokoa ho nts'etsopele ea embryonic, homeostasis ea batho ba baholo, le mofetše. Liphetoho tsa likokoana-hloko tsa likarolo tse 'maloa tsa tsela ea Wnt, tse kang Axin, APC, le ?-catenin, li ka lebisa ho oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of tankyrases (TNKS1 le TNKS2) e tsejoa ho thibela tsela ea Wnt ka ho eketsa botsitso ba Axin. |
| CPD100545 | KRP297 | KRP297, eo hape e tsejoang e le MK-0767 le MK-767, ke agonist ea PPAR e ka khonang ho phekola lefu la tsoekere la mofuta oa 2 le dyslipidemia. Ha e sebelisoa ho litoeba tsa ob/ob, KRP-297 (0.3 ho 10 mg/kg) e fokolitse tsoekere ea plasma le maemo a insulin 'me ea ntlafatsa ts'ebetso ea 2DG e sa sebetseng ea insulin ka har'a mesifa e le 'ngoe ka mokhoa o itšetlehileng ka tekanyo. Kalafo ea KRP-297 e thusa ho thibela nts'etsopele ea li-syndromes tsa lefu la tsoekere, hammoho le ho ntlafatsa phallo e sa sebetseng ea tsoekere ka har'a mesifa ea masapo. |
| CPD100543 | Inolitazone | Inolitazone, eo hape e tsejoang e le Efatutazone, CS-7017, le RS5444, ke sethibela sa molomo se fumanehang ka molomo sa PAPR-gamma se nang le ts'ebetso e ka bang teng ea antineoplastic. Inolitazone e tlama le ho kenya tšebetsong peroxisome proliferation-activated receptor gamma (PPAR-gamma), e leng se ka fellang ka ho kenngoa ha phapang ea lisele tsa tumor le apoptosis, hammoho le ho fokotsa ho ata ha lisele tsa tumor. PPAR-gamma ke receptor ea lihomone tsa nyutlelie le ligand-activated transcript factor e laolang polelo ea liphatsa tsa lefutso tse amehang lits'ebetsong tsa cellular joalo ka karohano, apoptosis, taolo ea potoloho ea lisele, carcinogenesis le ho ruruha. Sheba liteko tse sebetsang tsa tleliniki kapa liteko tse koetsoeng tsa bongaka u sebelisa moemeli enoa. (NCI Thesaurus) |
| CPD100541 | GW6471 | GW6471 ke mohanyetsi oa PPAR α (IC50 = 0.24 μ M). GW6471 e ntlafatsa kamano e tlamang ea sebaka se tlamang sa PPAR α ligand ho liprotheine tsa co-repressor SMRT le NCoR. |
| CPDD1537 | Lanifibranor | Lanifibranor, eo hape e tsejoang e le IVA-337, ke agonist ea peroxisome proliferator-activated receptors (PPAR). |
