nwamba # | Aha ngwaahịa | Nkọwa |
CPD100567 | GW501516 | GW501516 bụ PPARδ synthetic agonist nke na-egosiputa mmekọrịta dị elu maka PPARδ (Ki=1.1 nM) yana> 1000 fold selectivity n'elu PPARA na PPARγ. |
CPD100566 | GFT505 | Elafibranor, makwaara dị ka GFT-505, bụ PPARA/δ agonist abụọ. A na-amụ Elafibranoris ugbu a maka ọgwụgwọ ọrịa cardiometabolic gụnyere ọrịa shuga, nguzogide insulin, dyslipidemia, na ọrịa imeju na-adịghị egbu egbu (NAFLD). |
CPD100565 | Bavachinina | Bavachinina bụ akwụkwọ akụkọ okike pan-PPAR agonist sitere na mkpụrụ nke ahịhịa ahịhịa malaytea scurfpea nke China ọdịnala. Ọ na-egosi ọrụ siri ike na PPAR-γ karịa PPAR-α na PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l na 8.07 μmol/l na sel 293T, n'otu n'otu). |
CPD100564 | Troglitazone | Troglitazone, nke a makwaara dị ka CI991, bụ agonist PPAR nwere ike. Troglitazone bụ ọgwụ antidiabetic na mgbochi mkpali, yana onye otu thiazolidinediones nke ọgwụ. Edere ya maka ndị ọrịa nwere ọrịa shuga mellitus ụdị 2 na Japan Troglitazone, dị ka thiazolidinediones ndị ọzọ (pioglitazone na rosiglitazone), na-arụ ọrụ site na ịgbalite ndị na-anabata ihe na-eme proliferator (PPARs). Troglitazone bụ njikọ nke ma PPARA na - nke siri ike - PPARγ |
CPD100563 | Glabridin | Glabridin, otu n'ime phytochemicals na-arụ ọrụ na mpụta licorice, na-ejikọta ma na-arụ ọrụ njikọ njikọ njikọ nke PPARγ, yana onye na-anabata ya zuru oke. Ọ bụkwa onye nnabata GABAA mma modulator na-akwalite oxidation fatty acid na imeziwanye mmụta na ebe nchekwa. |
CPD100561 | Pseudoginsenoside-F11 | Pseudoginsenoside F11, ngwaahịa sitere n'okike dị na ginseng America mana ọ bụghị na ginseng Asia, bụ agonist PPARγ ọhụrụ. |
CPD100560 | Bezafibrate | Bezafibrate bụ agonist nke peroxisome proliferator-activated receptor alpha (PPARalpha) nwere ọrụ antilipidemic. Bezafibrate bụ ọgwụ fibrate a na-eji maka ọgwụgwọ hyperlipidemia. Bezafibrate na-ebelata ọkwa triglyceride, na-abawanye ọkwa cholesterol dị elu nke lipoprotein, ma na-ebelata mkpokọta lipoproteins dị ala. A na-erekarị ya dị ka Bezalip |
CPD100559 | GW0742 | GW0742, makwaara dị ka GW610742 na GW0742X bụ PPARδ/β agonist. GW0742 na-ebute ntozu oke akwara ozi nke Cortical Post-Mitotic Neurons. GW0742 na-egbochi ọbara mgbali elu, ọrịa vaskụla vaskụla na ọnọdụ oxidative, na arụ ọrụ endothelial na oke ibu nri kpatara. GW0742 nwere mmetụta nchebe kpọmkwem na hypertrophy obi ziri ezi.GW0742 nwere ike ịkwalite metabolism lipid na obi ma na vivo na in vitro. |
CPD100558 | Pioglitazone | Pioglitazone Hydrochloride bụ ngwakọta thiazolidinedione akọwara iji mepụta mmetụta mgbochi mkpali na antiarteriosclerotic. E gosiputara Pioglitazone iji gbochie mbufụt nke akwara ọbara nke L-NAME na-ebute na arteriosclerosis na iji gbochie ụbara TNF-α mRNA nke aspirin kpatara mmerụ ahụ mucosal gastric. Pioglitazone Hydrochloride bụ onye na-arụ ọrụ PPAR γ |
CPD100557 | Rosiglitazone | Rosiglitazone bụ ọgwụ antidiabetic na klas nke thiazolidinedione. Ọ na-arụ ọrụ dị ka onye na-ahụ maka insulin, site na ijikọ ndị na-anabata PPAR na sel abụba na ime ka mkpụrụ ndụ na-anabata insulin. Rosiglitazone bụ otu n'ime klas ọgwụ thiazolidinedione. Thiazolidinediones na-arụ ọrụ dị ka ndị na-ahụ maka insulin. Ha na-ebelata mkpokọta glucose, fatty acid na insulin n'ọbara. Ha na-arụ ọrụ site na ijikọ na ndị na-anabata proliferator-activated (PPARs). PPAR bụ ihe odide ederede na-ebi na nucleus wee bụrụ ndị ligands dị ka thiazolidinediones na-arụ ọrụ. Thiazolidinediones na-abanye n'ime cell, na-ejikọta na ndị na-anabata nuklia, ma gbanwee okwu nke mkpụrụ ndụ ihe nketa. |
CPD100556 | GSK0660 | GSK0660 bụ onye mmegide PPARδ ahọpụtara. GSK0660 na-ahazi transcript 273 dị iche iche na mkpụrụ ndụ TNFa a na-agwọ ma e jiri ya tụnyere TNFa naanị. Nyocha nke ụzọ gosipụtara mmụba nke cytokine-cytokine nnabata nnabata. Karịsịa, GSK0660 na-egbochi nkwalite TNFa na-ebute CCL8, chemokine na-etinye aka na mbanye leukocyte. GSK0660 na-egbochi mmetụta nke TNFα na nkwupụta nke cytokines na-etinye aka na nchịkọta leukocyte, gụnyere CCL8, CCL17, na CXCL10 na ọ nwere ike igbochi TNFa-induced retinal leukostasis. |
CPD100555 | Oroxin-A | Oroxin A, ihe na-arụ ọrụ dịpụrụ adịpụ na ahịhịa Oroxylum indicum (L.) Kurz, na-arụ ọrụ PPARγ ma na-egbochi α-glucosidase, na-arụ ọrụ antioxidant. |
CPD100546 | AZ-6102 | AZ6102 bụ ihe mgbochi TNKS1 / 2 nwere ike nke nwere 100-fold selectivity megide enzymes ezinụlọ PARP ndị ọzọ ma gosipụta 5 nM Wnt ụzọ mgbochi na sel DLD-1. Enwere ike ịhazi AZ6102 nke ọma na ngwọta intravenous dị mkpa nke ụlọ ọgwụ na 20 mg / mL, egosipụtala ezigbo pharmacokinetics na ụdị preclinical, ma gosipụta obere Caco2 efflux iji zere usoro nkwụsị nke tumor. Ụzọ Wnt canonical na-arụ ọrụ dị mkpa na mmepe embrayo, homeostasis anụ ahụ okenye, na ọrịa kansa. Mgbanwe germline nke ọtụtụ akụkụ ụzọ Wnt, dị ka Axin, APC, na ?-catenin, nwere ike ibute oncogenesis. Mgbochi nke poly (ADP-ribose) polymerase (PARP) catalytic ngalaba nke tankyrases (TNKS1 na TNKS2) mara na ọ ga-egbochi ụzọ Wnt site na nkwụsi ike nke Axin. |
CPD100545 | KRP297 | KRP297, makwaara dị ka MK-0767 na MK-767, bụ PPAR agonist nwere ike maka ọgwụgwọ ụdị ọrịa shuga 2 na dyslipidemia. Mgbe a na-enye ụmụ oke ob / ob, KRP-297 (0.3 ruo 10 mg / kg) belatara ọkwa glucose plasma na insulin ma kwalite nnabata 2DG nke na-eme ka insulin na-adịghị mma na akwara soleus n'ụzọ dabere na dose. Ngwọta KRP-297 bara uru iji gbochie mmepe nke ọrịa shuga na mgbakwunye na imeziwanye mbufe glucose na-adịghị mma na akwara skeletal. |
CPD100543 | Inolitazone | Inolitazone, nke a makwaara dị ka Efatutazone, CS-7017, na RS5444, bụ ihe mgbochi ọnụ nke PAPR-gamma nwere ike ime ya nwere ọrụ antineoplastic. Inolitazone na-ejikọta ma na-arụ ọrụ peroxisome proliferation-activated receptor gamma (PPAR-gamma), nke nwere ike ime ka mmepụta nke mkpụrụ ndụ tumor cell iche na apoptosis, yana ibelata mmụba nke cell tumor. PPAR-gamma bụ onye na-anabata homonụ nuklia na ihe ntinye ederede na-arụ ọrụ ligand na-achịkwa mkpụrụ ndụ ihe nketa na-etinye aka na usoro cellular dị ka ọdịiche, apoptosis, njikwa okirikiri cell, carcinogenesis, na mbufụt. Lelee maka nnwale ụlọ ọgwụ na-arụsi ọrụ ike ma ọ bụ nnwale ụlọ ọgwụ mechiri emechi site na iji nnọchite a. (NCI Thesaurus) |
CPD100541 | GW6471 | GW6471 bụ onye na-emegide PPAR α (IC50 = 0.24 μM). GW6471 na-akwalite njikọ njikọ nke ngalaba PPAR α ligand na protein protein SMRT na NCoR. |
CPDD1537 | Lanifibranor | Lanifibranor, nke a makwaara dị ka IVA-337, bụ agonist peroxisome proliferator-activated receptors (PPAR). |