| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD100567 | Saukewa: GW501516 | GW501516 wani agonist na musamman na PPARδ na roba wanda ke nuna babban kusanci ga PPARδ (Ki = 1.1 nM) tare da> zaɓin ninka 1000 akan PPARA da PPARγ. |
| Saukewa: CPD100566 | Saukewa: GFT505 | Elafibranor, wanda kuma aka fi sani da GFT-505, agonist ne na PPARA/δ dual. Elafibranoris a halin yanzu ana nazarin don maganin cututtukan cardiometabolic ciki har da ciwon sukari, juriya na insulin, dyslipidemia, da cututtukan hanta maras barasa (NAFLD). |
| Saukewa: CPD100565 | Bavachinina | Bavachinina wani labari ne na dabi'a na pan-PPAR agonist daga 'ya'yan itacen gargajiya na kasar Sin mai rage yawan glucose-lowing herb malaytea scurfpea. Yana nuna ayyuka masu ƙarfi tare da PPAR-γ fiye da PPAR-α da PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l da 8.07 μmol/l a cikin sel 293T, bi da bi). |
| Saukewa: CPD100564 | Troglitazone | Troglitazone, kuma aka sani da CI991, babban agonist na PPAR ne. Troglitazone magani ne na ciwon sukari da kuma maganin kumburi, kuma memba ne na rukunin magunguna na thiazolidinediones. An wajabta shi ga marasa lafiya da ke da nau'in ciwon sukari na 2 a cikin Japan Troglitazone, kamar sauran thiazolidinediones (pioglitazone da rosiglitazone), yana aiki ta hanyar kunna masu karɓa na proliferator (PPARs). Troglitazone shine haɗin gwiwa zuwa duka PPARA da - mafi ƙarfi - PPARγ |
| Saukewa: CPD100563 | Glabridin | Glabridin, ɗaya daga cikin phytochemicals masu aiki a cikin tsantsar licorice, yana ɗaure zuwa kuma yana kunna yankin ɗaurin ligand na PPARγ, da kuma cikakken mai karɓa. Hakanan madaidaicin mai karɓar mai karɓar GABAA ne mai haɓaka fatty acid oxidation da haɓaka koyo da ƙwaƙwalwa. |
| Saukewa: CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, samfurin halitta wanda aka samo a cikin ginseng na Amurka amma ba a cikin ginseng na Asiya ba, wani sabon abu ne na PPARγ agonist. |
| Saukewa: CPD100560 | Bezafibrate | Bezafibrate agonist ne na peroxisome proliferator-activated receptor alpha (PPARalpha) tare da aikin antilipidemic. Bezafibrate magani ne na fibrate da ake amfani dashi don maganin hyperlipidemia. Bezafibrate yana rage matakan triglyceride, yana ƙara yawan matakan lipoprotein cholesterol mai yawa, kuma yana rage jimla da ƙananan matakan lipoprotein cholesterol. Ana sayar da shi a matsayin Bezalip |
| Saukewa: CPD100559 | GW0742 | GW0742, kuma aka sani da GW610742 da GW0742X PPARδ/β agonist. GW0742 Yana haifar da Balagawar Jijiya na Farko na Cortical Post-Mitotic Neurons. GW0742 yana hana hauhawar jini, kumburin jijiyoyin bugun jini da matsayi na oxidative, da rashin aiki na endothelial a cikin kiba mai haifar da abinci. GW0742 yana da tasirin kariya kai tsaye akan hypertrophy na zuciya na dama.GW0742 na iya haɓaka metabolism na lipid a cikin zuciya duka a cikin vivo da in vitro. |
| Saukewa: CPD100558 | Pioglitazone | Pioglitazone Hydrochloride wani fili ne na thiazolidinedione wanda aka bayyana don samar da maganin kumburi da tasirin antiarteriosclerotic. An nuna Pioglitazone don hana L-NAME da ke haifar da kumburi na jijiyoyin jini da arteriosclerosis da kuma kawar da ƙarar TNF-a mRNA da aka samar ta hanyar aspirin-induced ciwon ciki mucosal rauni. Pioglitazone Hydrochloride shine mai kunnawa PPAR γ |
| Saukewa: CPD100557 | Rosiglitazone | Rosiglitazone maganin ciwon sukari ne a cikin rukunin magungunan thiazolidinedione. Yana aiki azaman mai karɓar insulin, ta hanyar ɗaure ga masu karɓar PPAR a cikin ƙwayoyin mai da kuma sa sel su zama masu karɓar insulin. Rosiglitazone memba ne na rukunin magungunan thiazolidinedione. Thiazolidinediones suna aiki azaman masu karɓar insulin. Suna rage glucose, fatty acid, da kuma adadin insulin na jini. Suna aiki ta hanyar ɗaure ga masu karɓa na proliferator-activated (PPARs). PPARs sune abubuwan rubutun da ke zaune a cikin tsakiya kuma suna kunna su ta hanyar haɗin gwiwa kamar thiazolidinediones. Thiazolidinediones suna shiga cikin tantanin halitta, suna ɗaure ga masu karɓar makaman nukiliya, kuma suna canza maganganun kwayoyin halitta. |
| Saukewa: CPD100556 | GSK0660 | GSK0660 zaɓin PPARδ antagonist. GSK0660 daban-daban da aka tsara 273 kwafi a cikin ƙwayoyin TNFa da aka yi wa magani idan aka kwatanta da TNFα kadai. Binciken hanya ya nuna wadatar siginar mai karɓa na cytokine-cytokine. Musamman, GSK0660 yana toshe haɓakar haɓakar TNFa na CCL8, chemokine da ke cikin ɗaukar leukocyte. GSK0660 yana toshe tasirin TNFa akan maganganun cytokines da ke cikin daukar ma'aikata na leukocyte, gami da CCL8, CCL17, da CXCL10 kuma yana iya toshe leukostasis na retinal na TNFa. |
| Saukewa: CPD10055 | Oroxin-A | Oroxin A, wani sashi mai aiki wanda aka ware daga ganye Oroxylum indicum (L.) Kurz, yana kunna PPARγ kuma yana hana α-glucosidase, yana yin aikin antioxidant. |
| Saukewa: CPD100546 | Saukewa: AZ-6102 | AZ6102 shine mai hanawa TNKS1/2 mai ƙarfi wanda ke da zaɓi na ninka 100 akan sauran enzymes iyali na PARP kuma yana nuna hanawar hanyar 5 nM Wnt a cikin sel DLD-1. AZ6102 za a iya tsara shi da kyau a cikin maganin asibiti mai dacewa a cikin 20 MG / mL, ya nuna magungunan pharmacokinetics masu kyau a cikin nau'i mai mahimmanci, kuma yana nuna ƙananan Caco2 efflux don kauce wa yiwuwar juriya na ƙwayoyin cuta. Hanyar Wnt ta canonical tana taka muhimmiyar rawa a cikin haɓakar amfrayo, homeostasis na nama na manya, da ciwon daji. Maye gurbi na ɓangarorin hanyoyin Wnt da yawa, kamar su Axin, APC, da ?-catenin, na iya haifar da cutar kansa. Hana poly (ADP-ribose) polymerase (PARP) catalytic yanki na tankyrases (TNKS1 da TNKS2) an san shi don hana hanyar Wnt ta hanyar haɓakar Axin. |
| Saukewa: CPD100545 | KRP297 | KRP297, wanda kuma aka sani da MK-0767 da MK-767, PPAR agonist mai yuwuwa don maganin ciwon sukari na 2 da dyslipidemia. Lokacin da aka gudanar da ob/ob mice, KRP-297 (0.3 zuwa 10 mg/kg) ya rage yawan glucose na plasma da matakan insulin kuma ya inganta haɓakar insulin-stimulated 2DG a cikin tsokar soleus ta hanyar dogaro da kashi. Jiyya na KRP-297 yana da amfani don hana haɓakar cututtukan ciwon sukari ban da haɓaka jigilar glucose mai rauni a cikin tsokar kwarangwal. |
| Saukewa: CPD100543 | Inolitazone | Inolitazone, wanda kuma aka sani da Efatutazone, CS-7017, da RS5444, mai hanawa na PAPR-gamma na baka tare da yuwuwar aikin antineoplastic. Inolitazone yana ɗaure zuwa kuma yana kunna gamma mai karɓa na proliferation-activated peroxisome (PPAR-gamma), wanda zai iya haifar da ƙaddamar da bambance-bambancen kwayar cutar tumo da apoptosis, da kuma raguwa a cikin ƙwayar ƙwayar ƙwayar cuta. PPAR-gamma shine mai karɓar hormone na nukiliya da ligand-activated transcription factor wanda ke sarrafa maganganun kwayoyin da ke cikin irin waɗannan hanyoyin salula kamar bambance-bambance, apoptosis, kula da sake zagayowar cell, carcinogenesis, da kumburi. Bincika gwaje-gwajen asibiti masu aiki ko rufaffiyar gwajin asibiti ta amfani da wannan wakili. (NCI Thesaurus) |
| Saukewa: CPD100541 | GW6471 | GW6471 PPAR α antagonist (IC50 = 0.24 μM). GW6471 yana haɓaka alaƙar ɗauri na yankin PPAR α ligand-ligand zuwa sunadaran haɗin gwiwar SMRT da NCoR. |
| Saukewa: CPDD1537 | Lanifibranor | Lanifibranor, wanda kuma aka sani da IVA-337, agonist ne na masu karɓar raɗaɗi (PPAR). |
