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Home >> Signaling Pathways >> Metabolism >> PPAR

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. GC42651 9-oxo-10(E),12(E)-Octadecadienoic Acid

    9-oxo ODA

     A natural agonist of PPARα
  3. GC42649 9-Nitrooleate

    9-硝基油酸

     A novel endogenous lipid signalling molecule
  4. GC41868 10-Nitrooleate

    10-硝基油酸,CXA-10

     A novel endogenous lipid signalling molecule
  5. GC41867 10-Nitrolinoleate

    10-LNO2, 10nitro9,12Octadecadienoic Acid, 10-NO2-LA

     A nitrated fatty acid and PPARγ agonist
  6. GC41530 4-oxo Docosahexaenoic Acid

    4-oxo DHA

     A putative DHA metabolite and PPARγ agonist
  7. GC41492 Edaglitazone

    依格列宗

     A PPARγ agonist
  8. GC41339 Pioglitazone Ketone

    吡格列酮

     An active metabolite of pioglitazone
  9. GC41102 15-deoxy-δ12,14-Prostaglandin D2

    15deoxyΔ12,14PGD2

     A metabolite of PGD2 and an agonist of DP2
  10. GC40838 (±)8(9)-EET methyl ester

    (±)8,9EpETrE methyl ester

     An esterified version of (±)8(9)-EET
  11. GC40764 CAY10514

    Methyl8hydroxy8(2pentyloxyphenyl)oct5ynoate

     A PPARα and PPARγ dual agonist
  12. GC40636 Amorfrutin A

    Amorfrutin 1

     An antidiabetic natural product
  13. GC40558 Hexanoyl Glycine

    己酰甘氨酸

     A urinary biomarker
  14. GC40440 (±)8(9)-EET

    (±)8,9EpETrE

     A racemic version of a CYP450 metabolite of arachidonic acid
  15. GC40384 CAY10410

    9,10dihydro15deoxyΔ12,14PGJ2, 9,10dihydro15deoxyΔ12,14Prostaglandin J2

     A less electrophilic, isosteric analog of 15-deoxy-D12,14-PGJ2
  16. GC19504 LJ570 LJ570 是一种 PPARα/PPARγ 双重激动剂，EC50 分别为 1.05 和 0.12 μM。
  17. GC33816 Ertiprotafib (PTP 112)

    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`；
  18. GC33780 RG-12525 (NID 525)

    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。
  19. GC33765 Palmitelaidic Acid (9-trans-Hexadecenoic acid)

    软脂酸; 9-trans-Hexadecenoic acid; trans-Palmitoleic acid

     A dietary fatty acid
  20. GC33734 Fonadelpar (NPS-005)

    NPS-005; SJP-0035

     Fonadelpar (NPS-005) 是 PPARδ；激动剂，用于神经麻痹性角膜病的研究。
  21. 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。
  22. GC32723 CDDO-Im (RTA-403)

    RTA-403; TP-235; CDDO-Imidazolide

     An activator of Nrf2 signaling
  23. GC32521 Imiglitazar (TAK-559)

    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。
  24. GC31693 Adelmidrol

    阿地米屈

     Adelmidrol is an analogue of palmitoylethanolamide (PEA) with anti-inflammatory activities.
  25. 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。
  26. 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。
  27. GC31552 Chiglitazar

    Carfloglitazar

     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。
  28. GC31532 Pparδ agonist 2 Pparδagonist2是一个PPARδ激动剂，来自专利WO2016057656A1。
  29. GC31510 Pparδ agonist PPARδagonist是PPARδ的激动剂，来自专利US20180071304，化合物实例10。
  30. GC31497 KD-3010 KD3010是一种具有口服活性的有效的选择性PPARδ激动剂。
  31. 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。
  32. GC31462 Arhalofenate (MBX 102)

    芳卤芬酯; MBX 102; JNJ 39659100

    A prodrug form of a PPARγ partial agonist
  33. 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。
  34. GC31451 Peliglitazar racemate (BMS 426707-01 racemate)

    BMS 426707-01 racemate

     Peliglitazar 外消旋体（BMS 426707-01 外消旋体）是 Peliglitazar 的外消旋体。
  35. GC31450 Naveglitazar racemate

    LY519818 racemate

     Naveglitazarracemate是Naveglitazar的外消旋体。Naveglitazar是过氧化物酶体增殖物激活受体(PPAR)α-γ双重，γ显性激动剂，在动物模型具有降低葡萄糖潜力。
  36. GC31408 Indeglitazar (PPM 204)

    PPM 204

     Indeglitazar (PPM 204) (PPM 204) 是一种可口服的 PPAR 泛激动剂，适用于所有三种 PPARα, PPARδ和PPARγ；。
  37. GC31396 Raspberry ketone (Frambione)

    覆盆子酮; Frambione; 4-(4-Hydroxyphenyl)-2-butanone

     Raspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity.
  38. GC31350 Astaxanthin

    虾青素

     Astaxanthin (β-Carotene-4,4'-dione, Trans-Astaxanthin), a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability. Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity.
  39. GC31325 Saroglitazar Magnesium

    沙罗格列扎镁盐

    Saroglitazarmagnesium是一种新型的过氧化物酶体增殖物活化受体PPAR的激动剂，具有显著PPARα活性和中度PPARγ活性,在HepG2细胞中的EC50值分别为0.65pMand3nM。
  40. GC30462 Pparδ agonist 1 Pparδagonist1是PPAR-δ的激动剂，EC50值为5.06nM，可用于研究与PPAR-δ相关的疾病，例如:线粒体疾病、肌肉疾病、血管疾病、脱髓鞘疾病和代谢疾病。
  41. GC30379 Saroglitazar

    沙罗格列扎

     A PPARα and PPARγ dual agonist
  42. GC19450 MA-0204 MA-0204 是一种有效的、高选择性和可口服的过氧化物酶体增殖物激活受体 δ (PPARδ) 调节剂，对人类、小鼠和大鼠 PPARδ 的 EC50 分别为 0.4 nM、7.9 nM 和 10 nM。
  43. GC19280 Pemafibrate

    佩玛贝特

     Pemafibrate (K-877) 是一种口服过氧化物酶体增殖物激活受体 (PPAR)-α 激动剂，用于治疗高脂血症，对 Gal4hPPARα 的 EC50 = 1 nM 。
  44. GC19242 Seladelpar

    MBX-8025

     Seladelpar (MBX-8025) 是一种口服有效的（50% 作用浓度 EC50 2 nM）和特异性 PPAR-δ 激动剂。
  45. GC18876 CAY10599 An agonist of PPARγ
  46. GC18151 Elafibranor (GFT505)

    GFT505

     An agonist of PPARα and PPARδ
  47. GC15909 RB394 A dual modulator of sEH and PPARγ
  48. GC16488 SR 2595 An inverse agonist of PPARγ
  49. GC15085 G3335

    G3335

     A PPARγ antagonist III
  50. GC14232 SR 1824 A non-agonist PPARγ ligand
  51. GC10190 DG-172 (hydrochloride) An orally available PPARβ/δ inverse agonist

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