| CAT # | Inoa Huahana | wehewehe |
| CPD100567 | GW501516 | ʻO GW501516 kahi agonist PPARδ-specific synthetic e hōʻike ana i ka pilina kiʻekiʻe no PPARδ (Ki = 1.1 nM) me ka> 1000 fold selectivity ma luna o PPARα a me PPARγ. |
| CPD100566 | GFT505 | ʻO Elafibranor, i kapa ʻia ʻo GFT-505, he pālua PPARα / δ agonist. Ke aʻo ʻia nei ʻo Elafibranoris no ka mālama ʻana i nā maʻi cardiometabolic e pili ana i ka maʻi diabetes, ka insulin resistance, dyslipidemia, a me ka maʻi momona momona ʻole (NAFLD). |
| CPD100565 | Bavachinina | ʻO Bavachinina kahi mea hou pan-PPAR agonist maoli mai ka hua o ka lāʻau malaytea scurfpea hoʻohaʻahaʻa i ka glucose mai Kina. Hōʻike ia i nā hana ikaika me ka PPAR-γ ma mua o ka PPAR-α a me ka PPAR-β/δ (EC50? =? 0.74 μmol/l, 4.00 μmol/l a me 8.07 μmol/l i loko o nā pūnaewele 293T, kēlā me kēia). |
| CPD100564 | Troglitazone | ʻO Troglitazone, i kapa ʻia ʻo CI991, kahi agonist PPAR ikaika. ʻO Troglitazone kahi lāʻau antidiabetic a anti-inflammatory, a he lālā o ka papa lāʻau o ka thiazolidinediones. Ua kuhikuhi ʻia no nā poʻe maʻi me ka maʻi diabetes type 2 ma Iapana Troglitazone, e like me nā thiazolidinediones ʻē aʻe (pioglitazone a me rosiglitazone), hana ma ka hoʻoulu ʻana i ka peroxisome proliferator-activated receptors (PPARs). He ligand ʻo Troglitazone i ka PPARα a - ʻoi aku ka ikaika - PPARγ |
| CPD100563 | ʻO Glabridin | ʻO Glabridin, kekahi o nā phytochemical ikaika i loko o ka licorice extract, hoʻopaʻa a hoʻōla i ka ligand binding domain o PPARγ, a me ka loaʻa ʻana o ka lōʻihi. ʻO ia kekahi GABAA receptor positive modulator e hoʻolaha ana i ka momona momona o ka momona a me ka hoʻomaikaʻi ʻana i ke aʻo ʻana a me ka hoʻomanaʻo. |
| CPD100561 | Pseudoginsenoside-F11 | ʻO Pseudoginsenoside F11, kahi huahana kūlohelohe i loaʻa i ka ginseng ʻAmelika akā ʻaʻole i loko o ka ginseng ʻĀsia, he agonist hapa PPARγ hou. |
| CPD100560 | ʻO Bezafibrate | ʻO Bezafibrate kahi agonist o ka peroxisome proliferator-activated receptor alpha (PPARalpha) me ka hana antilipidemic. ʻO Bezafibrate kahi lāʻau fibrate i hoʻohana ʻia no ka mālama ʻana i ka hyperlipidemia. Hoʻemi ʻo Bezafibrate i nā pae triglyceride, hoʻonui i ke kiʻekiʻe kiʻekiʻe o ka lipoprotein cholesterol kiʻekiʻe, a hoʻemi i ka nui a me ka haʻahaʻa lipoprotein cholesterol kiʻekiʻe. Kūʻai pinepine ʻia ʻo Bezalip |
| CPD100559 | GW0742 | ʻO GW0742, ʻike ʻia ʻo GW610742 a me GW0742X he agonist PPARδ/β. Hoʻoulu ʻo GW0742 i ka hoʻomaʻamaʻa mua ʻana o nā Neuronal Cortical Post-Mitotic Neurons. Kāohi ʻo GW0742 i ke kiʻekiʻe kiʻekiʻe, vascular inflammatory a me ke kūlana oxidative, a me ka endothelial dysfunction i ka momona i hoʻokomo ʻia i ka meaʻai. Loaʻa iā GW0742 nā hopena pale pono ma ka hypertrophy puʻuwai ʻākau. Hiki i ka GW0742 ke hoʻonui i ka metabolism lipid i loko o ka puʻuwai ma vivo a me in vitro. |
| CPD100558 | Pioglitazone | ʻO Pioglitazone Hydrochloride kahi pūhui thiazolidinedione i wehewehe ʻia e hana i nā hopena antiinflammatory a me antiarteriosclerotic. Hōʻike ʻia ʻo Pioglitazone e pale aku i ka ʻāʻī ʻana a me ka arteriosclerosis i hoʻokomo ʻia e L-NAME a me ka hoʻopaʻa ʻana i ka hoʻonui ʻana i ka TNF-α mRNA i hana ʻia e ka aspirin-induced gastric mucosal injury. ʻO Pioglitazone Hydrochloride kahi mea hoʻoikaika o PPAR γ |
| CPD100557 | ʻO Rosiglitazone | ʻO Rosiglitazone kahi lāʻau antidiabetic i ka papa thiazolidinedione o nā lāʻau lapaʻau. Hana ia ma ke ʻano he insulin sensitizer, ma ka hoʻopaʻa ʻana i nā mea loaʻa PPAR i loko o nā momona momona a me ka hoʻololi ʻana i nā cell i ka insulin. ʻO Rosiglitazone kahi lālā o ka papa thiazolidinedione o nā lāʻau lapaʻau. Hana ʻo Thiazolidinediones ma ke ʻano he insulin sensitizers. Hoʻemi lākou i ka glucose, fatty acid, a me ka nui o ke koko insulin. Hana lākou ma ka hoʻopaʻa ʻana i ka peroxisome proliferator-activated receptors (PPARs). ʻO nā PPAR nā mea transcription e noho ana i loko o ka nucleus a lilo i hoʻāla ʻia e nā ligands e like me thiazolidinediones. Hoʻokomo ʻo Thiazolidinediones i ke kelepona, hoʻopaʻa i nā mea hoʻokipa nuklea, a hoʻololi i ka ʻōlelo o nā genes. |
| CPD100556 | GSK0660 | ʻO GSK0660 kahi mea kū'ē PPARδ koho. ʻO GSK0660 i hoʻoponopono ʻokoʻa i nā transcripts 273 i nā cell TNFα-treated cell i hoʻohālikelike ʻia me TNFα wale nō. Ua hōʻike ʻia kahi loiloi ala i ka hoʻonui ʻana i ka hōʻailona hōʻailona cytokine-cytokine. Ma keʻano kūikawā, GSK0660 poloka i ka TNFα-induced upregulation o CCL8, he chemokine i komo i ka leukocyte recruitment. Hoʻopaʻa ʻo GSK0660 i ka hopena o TNFα ma nā hōʻike o nā cytokines i komo i ka leukocyte recruitment, me CCL8, CCL17, a me CXCL10 a no laila hiki iā ia ke pale i ka leukostasis retinal i hoʻokomo ʻia e TNFα. |
| CPD100555 | Oroxin-A | ʻO Oroxin A, kahi mea hana i hoʻokaʻawale ʻia mai ka herb Oroxylum indicum (L.) Kurz, hoʻāla i ka PPARγ a kāohi i ka α-glucosidase, e hana ana i ka hana antioxidant. |
| CPD100546 | AZ-6102 | ʻO AZ6102 kahi mea hoʻopaneʻe ikaika TNKS1 / 2 i loaʻa iā 100-fold selectivity e kūʻē i nā enzyme ʻohana PARP ʻē aʻe a hōʻike i ka pale ala 5 nM Wnt i nā pūnae DLD-1. Hiki ke hoʻolālā maikaʻi ʻia ʻo AZ6102 i loko o kahi hoʻonā intravenous pili i ke kino ma 20 mg/mL, ua hōʻike i ka pharmacokinetics maikaʻi i nā ʻano preclinical, a hōʻike i ka haʻahaʻa Caco2 efflux e pale aku i nā ʻano hana kūʻē ʻana i ka tumora. He kuleana koʻikoʻi ke ala Wnt canonical i ka ulu ʻana o ka embryonic, homeostasis ʻiʻo makua, a me ke kanesa. Hiki i nā hoʻololi Germline o kekahi mau ʻāpana ala Wnt, e like me Axin, APC, a me ?-catenin, hiki ke alakaʻi i ka oncogenesis. ʻO ka pale ʻana i ka poly (ADP-ribose) polymerase (PARP) catalytic domain o nā tankyrases (TNKS1 a me TNKS2) ua ʻike ʻia e kāohi i ke ala Wnt ma o ka hoʻonui ʻia ʻana o Axin. |
| CPD100545 | KRP297 | ʻO KRP297, i ʻike ʻia ʻo MK-0767 a me MK-767, he agonist PPAR hiki ke mālama ʻia i ka maʻi maʻi type 2 a me ka dyslipidemia. Ke hoʻohana ʻia i nā ʻiole ob / ob, KRP-297 (0.3 i ka 10 mg / kg) i hoʻemi i ka glucose plasma a me ka pae o ka insulin a hoʻomaikaʻi i ka hoʻopiʻi ʻana o ka insulin-hoʻoulu ʻia 2DG i loko o ka ʻiʻo soleus ma ke ʻano pili. He mea pono ka lapaʻau KRP-297 no ka pale ʻana i ka hoʻomohala ʻana o nā maʻi maʻi diabetic ma kahi o ka hoʻomaikaʻi ʻana i ka lawe ʻana i ka glucose impaired i loko o ka ʻiʻo iwi. |
| CPD100543 | Inolitazone | ʻO Inolitazone, ʻike ʻia hoʻi ʻo Efatutazone, CS-7017, a me RS5444, he mea hoʻopaneʻe PAPR-gamma waha me ka hana antineoplastic. Hoʻopili ʻo Inolitazone a hoʻōla i ka peroxisome proliferation-activated receptor gamma (PPAR-gamma), i hiki ke hopena i ka hoʻokomo ʻana i ka ʻokoʻa o ka cell tumo a me ka apoptosis, a me ka hōʻemi ʻana i ka hoʻonui ʻana o nā cell tumor. ʻO ka PPAR-gamma kahi mea hoʻokipa nuklea hormone a me ka ligand-activated transcription factor e hoʻomalu ana i ka hōʻike gene i loko o nā kaʻina cellular e like me ka hoʻokaʻawale ʻana, apoptosis, ka hoʻokele cell-cycle, carcinogenesis, a me ka mumū. E nānā no nā hoʻokolohua lapaʻau ikaika a i ʻole nā hoʻokolohua lapaʻau pani ʻia me ka hoʻohana ʻana i kēia mea hana. (NCI Thesaurus) |
| CPD100541 | GW6471 | ʻO GW6471 kahi mea kū'ē PPAR α (IC50 = 0.24 μ M). Hoʻonui ka GW6471 i ka pilina paʻa o ka PPAR α ligand-binding domain i nā protein co-repressor SMRT a me NCoR. |
| CPDD1537 | ʻO Lanifibranor | ʻO Lanifibranor, i kapa ʻia ʻo IVA-337, he peroxisome proliferator-activated receptors (PPAR) agonist. |
