PPAR(过氧化物酶体增殖剂激活受体)
The peroxisome proliferator-activated receptors (PPARs), belonging to the nuclear receptor superfamily, are a group of nuclear receptor proteins that are composed of three isoforms, including PPARγ, PPARα and PPARδ, encoded by separate genes. PPARs have a modular structure characterized by the presence of two highly conserved domains, including the DNA binding domain (DBD) of two zinc fingers and the ligand binding domain (LBD) of 13 α-helices and a small 4-stranded β-sheet. PPARs are ligand-regulated transcription factors controlling gene expression by binding to specific response elements (PPREs) within promoters, where PPARs bind as heterodimers with a retinoid X receptor and interact with cofactors upon binding leading to the increasing of rate of transcription initiation.
Products for PPAR
- Cat.No. 产品名称 Information
- GC35698 Ciprofibrate D6 An internal standard for the quantification of ciprofibrate
- GC35518 Bilobetin A biflavonoid with diverse biological activities
- GC35358 Ankaflavin Ankaflavin 是从Monascus-Fermented 红米中提取得到的,是PPARγ 的激动剂,具有抗炎活性。Ankaflavin 具有选择性的细胞毒性作用,诱导癌细胞死亡。
- GC35349 Angeloylgomisin H Angeloylgomisin H 是一种木脂素类化合物,可从五味子 (Schisandra rubriflora) 中提取。Angeloylgomisin H 通过激活 PPAR-γ 来改善胰岛素刺激的葡萄糖摄取潜力。
- GC35308 Alpinetin Alpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
- GC35281 Aleglitazar Aleglitazar(R1439; RO-0728804)是PPAR-α/γ激动剂,IC50分别为2.8 nM/4.6 nM。
- GC35143 4-O-Methyl honokiol A phenol with diverse biological activities
- GC44851 Rosiglitazone (potassium salt) A PPARγ agonist
- GC44645 Pioglitazone (potassium salt) A PPARγ agonist
- GC44191 MHY908 A PPARα and PPARγ dual agonist
- GC43880 Hydroxy Pioglitazone A major metabolite of pioglitazone
- GC43800 GW 9578 A potent, selective PPARα agonist
- GC43743 Gemfibrozil 1-O-β-Glucuronide A major metabolite of gemfibrozil
- GC43723 Galactosylsphingosine (d18:1) A bioactive sphingolipid
- GC43653 trans,trans-Farnesyl pyrophosphate ammonium salt An intermediate in sterol biosynthesis
- GC43180 CAY10592 A selective partial PPARδ agonist
- GC43174 CAY10573 A PPAR pan-agonist
- GC43162 CAY10506 A PPARγ agonist
- GC42890 Azelaoyl PAF A potent PPARγ agonist
- GC42791 Amorfrutin B A PPARγ agonist
- GC42651 9-oxo-10(E),12(E)-Octadecadienoic Acid A natural agonist of PPARα
- GC42649 9-Nitrooleate A novel endogenous lipid signalling molecule
- GC41868 10-Nitrooleate A novel endogenous lipid signalling molecule
- GC41867 10-Nitrolinoleate A nitrated fatty acid and PPARγ agonist
- GC41530 4-oxo Docosahexaenoic Acid A putative DHA metabolite and PPARγ agonist
- GC41492 Edaglitazone A PPARγ agonist
- GC41339 Pioglitazone Ketone An active metabolite of pioglitazone
- GC40764 CAY10514 A PPARα and PPARγ dual agonist
- GC40636 Amorfrutin A An antidiabetic natural product
- GC40558 Hexanoyl Glycine A urinary biomarker
- GC40384 CAY10410 A less electrophilic, isosteric analog of 15-deoxy-D12,14-PGJ2
- GC19504 LJ570 LJ570 是一种 PPARα/PPARγ 双重激动剂,EC50 分别为 1.05 和 0.12 μM。
- GC33816 Ertiprotafib (PTP 112) Ertiprotafib (PTP 112) 是 PTP1B,IkB 激酶 β 的抑制剂; (IKK-β) 和双 PPARα;和 PPARβ;激动剂,IC50 为 1.6 μ;M 代表 PTP1B,400 nM 代表 IKK-β;EC50 约为 1 μ;M 代表 PPARα;/PPAR`;
- GC33780 RG-12525 (NID 525) RG-12525 (NID 525) 是一种特异性、竞争性和口服有效的肽白三烯、LTC4、LTD4 和 LTE4 拮抗剂,抑制 LTC4、LTD4 和 LTE4 诱导的豚鼠实质条收缩,IC50 为 2.6 nM,2.5 nM和 7 nM,分别; RG-12525 (NID 525) 也是一种过氧化物酶体增殖物激活受体 gamma (PPAR-gamma) 激动剂,IC50 约为 60 nM,是 CYP3A4 的有效抑制剂,Ki 值为 0.5 μM。
- GC33765 Palmitelaidic Acid (9-trans-Hexadecenoic acid) A dietary fatty acid
- GC33734 Fonadelpar (NPS-005) Fonadelpar (NPS-005) 是 PPARδ;激动剂,用于神经麻痹性角膜病的研究。
- GC32933 NXT629 NXT629是一种有效、选择性、竞争性的PPAR-α拮抗剂,对人PPARα的IC50值为77nM,对其选择性高于对其他核激素受体,比如PPARδ,PPARγ,Erβ,GR和TRβ,IC50值分别为6.0,15,15.2,32.5和>100μM。NXT629具有高效抗癌作用,在动物模型试验中,能够抑制实验性癌细胞转移。
- GC32723 CDDO-Im (RTA-403) An activator of Nrf2 signaling
- GC32521 Imiglitazar (TAK-559) Imiglitazar (TAK-559) (TAK559) 是一种有效的双重人类 PPARα;和 PPARγ1 激动剂,EC50 值为 67 和 31 nM。
- GC31693 Adelmidrol Adelmidrol is an analogue of palmitoylethanolamide (PEA) with anti-inflammatory activities.
- GC31638 PPAR agonist 1 PPARagonist1是一种PPARα和PPARγ的激动剂,可用于降血糖、血脂水平、胆固醇和降低体重的研究。
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GC31623
PPARα-MO-1
PPARα-MO-1是有效的PPARα调节剂,来自专利WO/2004/110982A1,结构式I。
- GC31552 Chiglitazar Chiglitazar是泛过氧化物酶体增殖物激活受体(PPARα/γ)的双抑制剂,其对PPARα,PPARγ和PPARδ的EC50值分别为1.2,0.08和1.7μM。
- GC31532 Pparδ agonist 2 Pparδagonist2是一个PPARδ激动剂,来自专利WO2016057656A1。
- GC31510 Pparδ agonist PPARδagonist是PPARδ的激动剂,来自专利US20180071304,化合物实例10。
- GC31497 KD-3010 KD3010是一种具有口服活性的有效的选择性PPARδ激动剂。
- GC31471 GSK376501A GSK376501A是一种选择性的过氧化物酶体增殖物激活受体γ(PPARγ)调节剂。可用于治疗2型糖尿病。
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GC31462
Arhalofenate (MBX 102)
A prodrug form of a PPARγ partial agonist
- GC31452 AVE-8134 AVE-8134是PPARα的有效激动剂,对人体和啮齿类动物的PPARα的EC50值分别为100和3000nM。
- GC31451 Peliglitazar racemate (BMS 426707-01 racemate) Peliglitazar 外消旋体(BMS 426707-01 外消旋体)是 Peliglitazar 的外消旋体。