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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

  1. Cat.No. 产品名称 Information
  2. GC35698 Ciprofibrate D6 An internal standard for the quantification of ciprofibrate
  3. GC35518 Bilobetin A biflavonoid with diverse biological activities
  4. 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。
  5. 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。
  6. 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.
  7. GC35281 Aleglitazar Aleglitazar(R1439; RO-0728804)是PPAR-α/γ激动剂,IC50分别为2.8 nM/4.6 nM。
  8. GC35143 4-O-Methyl honokiol A phenol with diverse biological activities
  9. GC44851 Rosiglitazone (potassium salt) A PPARγ agonist
  10. GC44645 Pioglitazone (potassium salt) A PPARγ agonist
  11. GC44191 MHY908 A PPARα and PPARγ dual agonist
  12. GC43880 Hydroxy Pioglitazone A major metabolite of pioglitazone
  13. GC43800 GW 9578 A potent, selective PPARα agonist
  14. GC43743 Gemfibrozil 1-O-β-Glucuronide A major metabolite of gemfibrozil
  15. GC43723 Galactosylsphingosine (d18:1) A bioactive sphingolipid
  16. GC43653 trans,trans-Farnesyl pyrophosphate ammonium salt An intermediate in sterol biosynthesis
  17. GC43180 CAY10592 A selective partial PPARδ agonist
  18. GC43174 CAY10573 A PPAR pan-agonist
  19. GC43162 CAY10506 A PPARγ agonist
  20. GC42890 Azelaoyl PAF A potent PPARγ agonist
  21. GC42791 Amorfrutin B A PPARγ agonist
  22. GC42651 9-oxo-10(E),12(E)-Octadecadienoic Acid A natural agonist of PPARα
  23. GC42649 9-Nitrooleate A novel endogenous lipid signalling molecule
  24. GC41868 10-Nitrooleate A novel endogenous lipid signalling molecule
  25. GC41867 10-Nitrolinoleate A nitrated fatty acid and PPARγ agonist
  26. GC41530 4-oxo Docosahexaenoic Acid A putative DHA metabolite and PPARγ agonist
  27. GC41492 Edaglitazone A PPARγ agonist
  28. GC41339 Pioglitazone Ketone An active metabolite of pioglitazone
  29. GC40764 CAY10514 A PPARα and PPARγ dual agonist
  30. GC40636 Amorfrutin A An antidiabetic natural product
  31. GC40558 Hexanoyl Glycine A urinary biomarker
  32. GC40384 CAY10410 A less electrophilic, isosteric analog of 15-deoxy-D12,14-PGJ2
  33. GC19504 LJ570 LJ570 是一种 PPARα/PPARγ 双重激动剂,EC50 分别为 1.05 和 0.12 μM。
  34. 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`;
  35. 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。
  36. GC33765 Palmitelaidic Acid (9-trans-Hexadecenoic acid) A dietary fatty acid
  37. 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。
  38. 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。
  39. GC32723 CDDO-Im (RTA-403) An activator of Nrf2 signaling
  40. 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。
  41. GC31693 Adelmidrol Adelmidrol is an analogue of palmitoylethanolamide (PEA) with anti-inflammatory activities.
  42. 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。
  43. 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。

  44. 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。
  45. GC31532 Pparδ agonist 2 Pparδagonist2是一个PPARδ激动剂,来自专利WO2016057656A1。
  46. GC31510 Pparδ agonist PPARδagonist是PPARδ的激动剂,来自专利US20180071304,化合物实例10。
  47. GC31497 KD-3010 KD3010是一种具有口服活性的有效的选择性PPARδ激动剂。
  48. 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。
  49. GC31462 Arhalofenate (MBX 102)

    A prodrug form of a PPARγ partial agonist

  50. 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。
  51. 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。

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