human pparα

Tesaglitazar 是一种有效且具有选择性的过氧化物 PPAR α γ受体双重激动剂，对 PPARγ的亲和力比 PPARα更有效，对大鼠PPARα和人PPARα的EC50分别为13.4 μM 和3.6 μM,对大鼠PPARγ和人类 PPARγ的EC50都是0.2 μM。Tesaglitazar 诱导大鼠皮下组织间质间充质细胞DNA 合成和纤维肉瘤形成。

LY518674 (LY-674) 是一种高效、选择性的 PPARα 激动剂，对人 PPARα 作用的 EC50 值为 42 nM。LY518674 能降低甘油三酸酯，增加 HDL-C，可用于研究动脉粥样硬化。

Muraglitazar (BMS-298585) 是一种 PPAR α γ的双激动剂，用于治疗2型糖尿病及相关血脂异常。Muraglitazar 对人 PPARα (EC50 = 320 nM)和 PPARγ(EC50 = 110 nM)具有较强的体外活性。

Pioglitazone hydrochloride (AD 4833) 是一种选择性PPARγ激动剂，高亲和力结合到 PPARγ 配体结合域。作用于人和鼠 PPARγ，EC50分别为 0.93 和 0.99 μM。它是一种口服活性噻唑烷二酮的盐酸盐，具有抗糖尿病特性和潜在的抗肿瘤活性。

Pioglitazone (U 72107) 是一种胰岛素增敏剂和噻唑烷二酮，适用于治疗 2 型糖尿病。它是一种选择性PPARγ激动剂，高亲和力结合到 PPARγ 配体结合域，作用于人和鼠 PPARγ的EC50分别为 0.93 和 0.99 μM。

Aleglitazar (R1439) 是一种高效的 PPARα γ 双重激动剂，对人 PPARα 和 PPARγ 作用的 IC50 分别为 38 nM 和 19 nM。Aleglitazar 可用于 II 型糖尿病的研究。

Clofibrate (Clofibrato) 是芳氧基异丁酸衍生物，具有抗高血脂活性。它是一种 PPAR 的激动剂，对人和鼠 PPARα 和 PPARγ 的 EC50值分别为 55 μM，约500 μM 和 50 μM，约500 μM。

Bezafibrate (BM15075) 是一种降血脂剂，是PPAR 的激动剂，对人以及鼠PPARα、PPARγ和PPARδ的EC50分别为 50、60和20 μM， 以及 90、55 和110 μM。

GW0742 是一种有效且特异性的 PPARδ 激动剂，对人 PPARδ、PPARα 和 PPARγ 的 EC50值分别为 1、1.1 和 2 μM。

GW 7647 是一种有效且高度选择性的 PPAR α 激动剂，人 PPAR α、PPAR γ 和 PPAR δ 受体的 EC 50 值分别为 6、1100 和 6200 nM ）。GW 7647 能减少巨噬细胞中一氧化氮的产生，在体内有降脂和抗炎特性。

BMS-687453 是一种选择性 PPARα激动剂，对人 PPARα的 EC50和 IC50分别为 10 nM 和 260 nM。它较弱地抑制 PPARγ 的活性，EC50和 IC50值分别为 4100 nM 和大于 15000 nM。

CUDA 是一种可溶性环氧水解酶抑制剂，对小鼠 sEH 和人 sEH 作用的 IC50分别为 11.1 和 112 nM。它能选择性地上调过氧化物酶体增殖激活受体 PPARα的活性，有用于心血管疾病的研究潜力。

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-conjugated linoleic acid reduces serum fasting glucose, insulin, and triglyceride levels and decreases white adipose tissue macrophage infiltration inob obmice. It also increases body weight gain and body fat in weanling mice.4[Matreya, LLC. Catalog No. 1278] 1.Shultz, T.D., Chew, B.P., Seaman, W.R., et al.Inhibitory effect of conjugated dienoic derivatives of linoleic acid and β-carotene on the in vitro growth of human cancer cellsCancer Lett.63(2)125-133(1992) 2.Moya-Camarena, S.Y., Heuvel, J.P.V., Blanchard, S.G., et al.Conjugated linoleic acid is a potent naturally occurring ligand and activator of PPARαJ. Lipid Res.40(8)1426-1433(1999) 3.Moloney, F., Toomey, S., Noone, E., et al.Antidiabetic effects of cis-9, trans-11-conjugated linoleic acid may be mediated via anti-inflammatory effects in white adipose tissueDiabetes56(3)574-582(2007) 4.Pariza, M.W., Park, Y., and Cook, M.E.The biologically active isomers of conjugated linoleic acidProg. Lipid Res.40(4)283-298(2001)

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.

AVE-8134 is an agonist of PPARα. For human and rodent PPARα receptor, the EC50 values are 100 and 3000 nM, respectively.

CP-868388 free base (CP-868388) 是一种具有口服活性、有效性和选择性的 PPARα 激动剂，具有降血脂和抗炎活性，可用于研究血脂异常。

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

Oleoylethanolamide (N-Oleoylethanolamide) 是一种PPAR-α 的高亲和力内源性激动剂，可用于肥胖和动脉硬化的相关研究。

Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2.5 µM时诱导这些细胞类型的自噬细胞死亡。DDA (0.37 µg/kg)在B16/F10小鼠黑色素瘤模型和TS/A小鼠乳腺癌模型中减缓肿瘤生长，并在体内外诱导癌细胞分化。

20-HEPE is a metabolite of eicosapentaenoic acid that is formed via ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. It activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter when used at a concentration of 10 μM. 20-HEPE also activates murine transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks antinociceptive activity in rats.

BMS-711939 is a potent and specific peroxisome proliferator-activated receptor (PPARα) agonist that has demonstrated excellent efficacy and safety in vivo in preclinical studies with an EC50 of 4 nM for PPARα in humans.

NXT629 是一种具有选择性和高效性的 PPAR-α 拮抗剂，具有抗癌活性，抑制 PPARδ，PPARγ，Erβ，GR 和 TRβ，可用于研究卵巢癌和黑色素瘤。

GW 9578 是一种具有选择性和有效性的 PPARα 激动剂 ，具有有效的降脂活性，可用于研究牛皮癣，关节炎，脱发，哮喘和I型糖尿病。

Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 |Nugent et al (2001) Potentiation of glucose uptake in 3T3-L1 adipocytes by PPARγ agonists is maintained in cells expressing a PPARγ dominant-negative mutant: evidence for selectivity in the downstream responses to PPARγ activation. Mol.Endocrinol. 15 1729 PMID:11579205 |Way et al (2001) Adipose tissue resistin expression is severely suppressed in obesity and stimulated by peroxisome proliferator-activated receptor γ agonists. J.Biol.Chem. 276 25651 PMID:11373275