PPAR

信号通路图

研究领域

抑制剂选择性比较

特异性亚型抑制剂

PPAR产品

所有产品 PPAR抑制剂(9) PPAR激活剂(10) PPAR拮抗剂(3) PPAR激动剂(20) PPAR调节剂(4)

目录号	产品描述	文献引用	实验数据
S2871	T0070907 T0070907是一种有效的，选择性PPARγ抑制剂，无细胞试验中IC50为1 nM，比作用于PPARα和PPARδ选择性高800倍以上。T0070907 在ME-180和SiHa细胞中可显著降低 DNA-PKcs 和 RAD51 蛋白的表达水平。	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 J Cell Mol Med, 2020, 10.1111/jcmm.15783	Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
S7767	AZ6102 AZ6102是有效的TNKS1/2抑制剂，选择性比作用于其他PARP家族的激酶高100倍，其在DLD-1细胞中抑制Wnt信号通路（IC50为5 nM）。	Nat Commun, 2019, 10(1):4898
S2798	GW6471 GW 6471 是一种 PPARα 的有效拮抗剂，其IC50值为0.24 μM。
S7484	FH535 FH535是一种Wnt/β-catenin信号传导抑制剂，同时也是PPARγ和PPARδ的双重拮抗剂。	Sci Rep, 2020, 10(1):15837 Gastroenterology, 2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc, 2019, 3(7):1246-1260	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
S5824	Cinnamyl alcohol Cinnamyl alcohol是一种存在于肉桂中的天然产物。
S5113	Propyl gallate Propyl gallate is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527	Fenofibric acid Fenofibric acid是一种降脂剂，降低低密度脂蛋白胆固醇和甘油三脂。	Int J Pharm, 2019, 570:118661
S9129	20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 是从红参中提取的主要生物活性化合物之一，在世界范围内，红参已越来越多地用于增强认知和身体健康。它具有抗发炎、抗氧化、免疫调节作用和对神经系统有积极作用的有效特性。20(S)-Ginsenoside Rh1 可抑制 PPAR-γ、TNF-α、IL-6 和 IL-1β 的表达。
S7867	Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。
S3290^New	Procyanidin B2 Procyanidin B2 (PCB2) 是一种存在于常见食品中的天然类黄酮，具有抗炎、抗氧化和抗癌活性。Procyanidin B2 可激活 PPARγ 并诱导小鼠巨噬细胞M2极化。Procyanidin B2 可显著抑制百草枯在大鼠模型中肺组织中 NLRP3 炎性小体的活化。
S8029	WY-14643 (Pirinixic Acid) WY 14643 (Pirinixic Acid, NSC 310038) 是一种有效的过氧化物酶体增殖子和PPARα激活剂，EC50为1.5 μM。	Genes Dev, 2020, 34(7-8):526-543 Environ Pollut, 2020, 29;264:114659 Biomed Pharmacother, 2020, 127:110155	(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
S1729	Gemfibrozil Gemfibrozil (CI-719) 是一种降低血脂水平的化合物。
S1849	Daidzein Daidzein属于异黄酮类。	J Mol Neurosci, 2018, 64(2):211-223
S9189	Oroxin A Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S5121	Phytol Phytol, a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S3875	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.
S5851	4'-Methoxychalcone 4'-Methoxychalcone存在于柑橘属植物中，是一种查耳酮衍生物，具有多种药理活性，如抗肿瘤和消炎活性。
S4708	Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) 是一种内源性的脂肪酸酰胺，能在体外选择性激活PPAR-α，EC50为3.1±0.4 μM。	J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177	Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
S2915	GW9662 GW9662是一种选择性PPAR拮抗剂，作用于PPARγ，无细胞试验中IC50为3.3 nM，在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。	J Exp Clin Cancer Res, 2020, 39(1):24 Signal Transduct Target Ther, 2020, 4;5(1):20 Transl Stroke Res, 2020, 10.1007/s12975-020-00842-9	Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
S8025	GSK3787 GSK3787是一种选择性的，不可逆PPARδ拮抗剂，pIC50为6.6，对hPPARα和hPPARγ没有亲和力。	Theranostics, 2019, 9(12):3501-3514 Nat Med, 2018, 24(3):360-367 Neuropharmacology, 2017, 113(Pt A):396-406	PPARβ/δ activation protects against corticosterone-induced astrocyte damage. (a) Astrocytes treated with Cort at concentrations of 1, 10, and 100 μM( n = 4; F = 329.412 > F0.01 (3, 12); P < 0.01 vs. Con group); (b) MTT assay performed 24 hours after treatment with Cort (10 μM) and GW (0.1, 1, and 10 μM) (n = 5; F = 7.402 > F 0.01 (4, 20); P < 0.01 vs. Con group; #P < 0.05 vs. Cort. group); (c) MTT assay performed after 24 hours of treatment with Cort (10 μM), GW (10 μM), and GSK (10 μM) (n = 4; F = 42.431 > F0.01 (3, 12); P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (d) MTT assay performed 24 hours after treatment with GSK (0.1, 1, and 10 μM) (n = 4; F = 1.659 < F0.01 (3, 12); P > 0.05 vs. Con group); (e) PPARβ/δ expression levels measured by RT-qPCR (n = 4; F = 27.018 > F0.01 (3, 12); P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group); (f) PPARβ/δ expression levels measured by Western blot (n = 4; F = 34.723 > F0.01 (3, 12); **P < 0.01vs. Con group; ##P < 0.01 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey’s multiple comparisons test. Each data point represents the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787.
S5817	GSK0660 GSK0660是有效的PPARβ/δ拮抗剂，pIC50为6.8。在浓度高达近于10 μM时，对PPARα和PPARγ没有活性。	Nat Commun, 2019, 11;10(1):4621
S2505	Rosiglitazone maleate Rosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药，是PPARγ的高亲和、选择性的激动剂，IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。	Cell Death Dis, 2020, 11(9):752 Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4	Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast.
S2556	Rosiglitazone Rosiglitazone (BRL 49653) 是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。	Nat Commun, 2020, 11(1):71 Cell Death Dis, 2020, 11(9):752 Cancer Cell Int, 2020, 19;20:58
S2590	Pioglitazone Pioglitazone 是一种选择性过氧化物酶体增殖物激活受体γ (PPARγ) 激动剂，用于治疗糖尿病。是全长hPPARα的弱激活剂，对全长hPPARδ没有作用。	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 FEBS J, 2020, 287(3):529-545	PPARγ activation, but not PPARα activation, increases β-klotho expression and FGF21 signaling. Protein (A) levels of β-klotho in hepatocytes after stimulation with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h
S8020	GW0742 GW0742是一种有效的，选择性PPARβ/δ激动剂，IC50为1 nM，比作用于hPPARα和hPPARγ选择性高1000倍。	Cells, 2019, 8(12) Int J Med Sci, 2019, 16(12):1593-1603 Sci Rep, 2017, 7:45234	(b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787
S2046	Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂，对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。	Biol Pharm Bull, 2019, 42(8):1303-1309 Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2665	Ciprofibrate Ciprofibrate (Win-35833)是一种过氧化物酶体增殖物激活受体激动剂。	Respir Physiol Neurobiol, 2020, 271:103290
S4159	Bezafibrate Bezafibrate (BM 15075) 是第一个临床测试的双重pan-peroxisome proliferator-activated receptors (PPAR)（过氧化物酶体增殖物激活受体）联合激动剂。
S4207	Clofibric Acid Clofibric acid 是PPARα激动剂，是一种降血脂剂。
S1794	Fenofibrate Fenofibrate 是一种Fibrate类化合物，是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂，EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ，对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。	J Cell Mol Med, 2020, 24(6):3384-3398 Cancer Discov, 2020, CD-20-0160 Int J Biol Macromol, 2019, 134:759-769	E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
S2075	Rosiglitazone HCl Rosiglitazone HCl是一种降血糖药物，通过在脂肪细胞中与PPAR受体结合而刺激胰岛素分泌。	Cell Death Dis, 2020, 11(9):752 Reprod Toxicol, 2016, 61:162-8 Toxicol Appl Pharmacol, 2015, 285(1):51-60
S9199	Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S8770	Lanifibranor (IVA-337) Lanifibranor (IVA-337)是一种泛PPAR激动剂，对hPPARα、hPPARδ 和 hPPARγ的EC50值分别为1537 nM、866 nM和206 nM。
S3846	Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity.	Clin Exp Reprod Med, 2020, 47(2):108-113
S3786	Glabridin Glabridin, one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
S8432	Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂，PPAR是配体激活的转录因，可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。	Nat Commun, 2019, 11;10(1):4621
S3878	Bavachinin Bavachinin (7-O-Methylbavachin) ia a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S5812	Choline Fenofibrate Choline fenofibrate是一种非诺贝特酸的胆碱盐，非诺贝特酸是一种合成的苯氧异丁酸衍生物，具有抗高血脂活性，是PPARα激动剂。
S3720	Elafibranor Elafibranor (GFT505) 是PPAR-alpha和PPAR-δ的激动剂，改善胰岛素敏感度、有益于葡萄糖稳态、脂质代谢并减少炎症。
S9480	Raspberry Ketone Raspberry ketone是一种天然存在的酚类化合物，是红莓中的主要芳香化合物。
S5615	Cardarine (GW501516) Cardarine (GW501516, Cardarine, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
S6906^New	Capric acid Capric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分，可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围，产品可能是固体、液体或半固体状态。
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
S3834	Astaxanthin Astaxanthin, a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability.	Aging (Albany NY), 2019, 11(22):10513-10531 Nature, 2018, 560(7718):372-376
S3868	Harmine Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.	Cell Death Dis, 2019, 10(12):899

目录号	产品描述	文献引用	实验数据
S2871	T0070907 T0070907是一种有效的，选择性PPARγ抑制剂，无细胞试验中IC50为1 nM，比作用于PPARα和PPARδ选择性高800倍以上。T0070907 在ME-180和SiHa细胞中可显著降低 DNA-PKcs 和 RAD51 蛋白的表达水平。	Cancer Lett,2020, 476:34-47 Front Immunol,2020, 11:1224 J Cell Mol Med,2020, 10.1111/jcmm.15783	Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
S7767	AZ6102 AZ6102是有效的TNKS1/2抑制剂，选择性比作用于其他PARP家族的激酶高100倍，其在DLD-1细胞中抑制Wnt信号通路（IC50为5 nM）。	Nat Commun,2019, 10(1):4898
S2798	GW6471 GW 6471 是一种 PPARα 的有效拮抗剂，其IC50值为0.24 μM。
S7484	FH535 FH535是一种Wnt/β-catenin信号传导抑制剂，同时也是PPARγ和PPARδ的双重拮抗剂。	Sci Rep,2020, 10(1):15837 Gastroenterology,2019, 10.1053/j.gastro.2019.11.013 J Endocr Soc,2019, 3(7):1246-1260	Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
S5824	Cinnamyl alcohol Cinnamyl alcohol是一种存在于肉桂中的天然产物。
S5113	Propyl gallate Propyl gallate is an antioxidant used in foods especially animal fats and vegetable oils, also in a wide variety of cosmetics and beauty care products.
S4527	Fenofibric acid Fenofibric acid是一种降脂剂，降低低密度脂蛋白胆固醇和甘油三脂。	Int J Pharm,2019, 570:118661
S9129	20(S)-Ginsenoside Rh1 20(S)-Ginsenoside Rh1 是从红参中提取的主要生物活性化合物之一，在世界范围内，红参已越来越多地用于增强认知和身体健康。它具有抗发炎、抗氧化、免疫调节作用和对神经系统有积极作用的有效特性。20(S)-Ginsenoside Rh1 可抑制 PPAR-γ、TNF-α、IL-6 和 IL-1β 的表达。
S7867	Oleuropein Oleuropein 是一种从橄榄叶中分离出的抗氧化多酚。Oleuropein 具有抗氧化、抗炎和抗动脉粥样硬化的作用，并在体外抑制脂肪细胞的分化。Oleuropein 抑制 PPARγ 活性。Oleuropein 通过直接抑制PPARγ转录活性发挥抗脂肪形成作用。Oleuropein 还可抑制aromatase。Oleuropein 可诱导凋亡。Phase 2。

目录号	产品描述	文献引用	实验数据
S3290^New	Procyanidin B2 Procyanidin B2 (PCB2) 是一种存在于常见食品中的天然类黄酮，具有抗炎、抗氧化和抗癌活性。Procyanidin B2 可激活 PPARγ 并诱导小鼠巨噬细胞M2极化。Procyanidin B2 可显著抑制百草枯在大鼠模型中肺组织中 NLRP3 炎性小体的活化。
S8029	WY-14643 (Pirinixic Acid) WY 14643 (Pirinixic Acid, NSC 310038) 是一种有效的过氧化物酶体增殖子和PPARα激活剂，EC50为1.5 μM。	Genes Dev, 2020, 34(7-8):526-543 Environ Pollut, 2020, 29;264:114659 Biomed Pharmacother, 2020, 127:110155	(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
S1729	Gemfibrozil Gemfibrozil (CI-719) 是一种降低血脂水平的化合物。
S1849	Daidzein Daidzein属于异黄酮类。	J Mol Neurosci, 2018, 64(2):211-223
S9189	Oroxin A Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S5121	Phytol Phytol, a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.
S3875	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.
S5851	4'-Methoxychalcone 4'-Methoxychalcone存在于柑橘属植物中，是一种查耳酮衍生物，具有多种药理活性，如抗肿瘤和消炎活性。
S4708	Palmitoylethanolamide Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) 是一种内源性的脂肪酸酰胺，能在体外选择性激活PPAR-α，EC50为3.1±0.4 μM。	J Steroid Biochem Mol Biol, 2019, 10.1016/j.jsbmb.2018.07.005
S9177	Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.

目录号	产品描述	文献引用	实验数据
S2915	GW9662 GW9662是一种选择性PPAR拮抗剂，作用于PPARγ，无细胞试验中IC50为3.3 nM，在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。	J Exp Clin Cancer Res, 2020, 39(1):24 Signal Transduct Target Ther, 2020, 4;5(1):20 Transl Stroke Res, 2020, 10.1007/s12975-020-00842-9	Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
S8025	GSK3787 GSK3787是一种选择性的，不可逆PPARδ拮抗剂，pIC50为6.6，对hPPARα和hPPARγ没有亲和力。	Theranostics, 2019, 9(12):3501-3514 Nat Med, 2018, 24(3):360-367 Neuropharmacology, 2017, 113(Pt A):396-406	PPARβ/δ activation protects against corticosterone-induced astrocyte damage. (a) Astrocytes treated with Cort at concentrations of 1, 10, and 100 μM( n = 4; F = 329.412 > F0.01 (3, 12); P < 0.01 vs. Con group); (b) MTT assay performed 24 hours after treatment with Cort (10 μM) and GW (0.1, 1, and 10 μM) (n = 5; F = 7.402 > F 0.01 (4, 20); P < 0.01 vs. Con group; #P < 0.05 vs. Cort. group); (c) MTT assay performed after 24 hours of treatment with Cort (10 μM), GW (10 μM), and GSK (10 μM) (n = 4; F = 42.431 > F0.01 (3, 12); P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (d) MTT assay performed 24 hours after treatment with GSK (0.1, 1, and 10 μM) (n = 4; F = 1.659 < F0.01 (3, 12); P > 0.05 vs. Con group); (e) PPARβ/δ expression levels measured by RT-qPCR (n = 4; F = 27.018 > F0.01 (3, 12); P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group); (f) PPARβ/δ expression levels measured by Western blot (n = 4; F = 34.723 > F0.01 (3, 12); **P < 0.01vs. Con group; ##P < 0.01 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey’s multiple comparisons test. Each data point represents the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787.
S5817	GSK0660 GSK0660是有效的PPARβ/δ拮抗剂，pIC50为6.8。在浓度高达近于10 μM时，对PPARα和PPARγ没有活性。	Nat Commun, 2019, 11;10(1):4621

目录号

产品描述

文献引用

实验数据

S2915

GW9662

GW9662是一种选择性PPAR拮抗剂，作用于PPARγ，无细胞试验中IC50为3.3 nM，在细胞中作用于PPARγ比作用于PPARα和PPARδ的功能选择性强10到600倍。

J Exp Clin Cancer Res, 2020, 39(1):24

Signal Transduct Target Ther, 2020, 4;5(1):20

Transl Stroke Res, 2020, 10.1007/s12975-020-00842-9

S8025

GSK3787

GSK3787是一种选择性的，不可逆PPARδ拮抗剂，pIC50为6.6，对hPPARα和hPPARγ没有亲和力。

Theranostics, 2019, 9(12):3501-3514

Nat Med, 2018, 24(3):360-367

Neuropharmacology, 2017, 113(Pt A):396-406

S5817

GSK0660

GSK0660是有效的PPARβ/δ拮抗剂，pIC50为6.8。在浓度高达近于10 μM时，对PPARα和PPARγ没有活性。

Nat Commun, 2019, 11;10(1):4621

目录号	产品描述	文献引用	实验数据
S2505	Rosiglitazone maleate Rosiglitazone maleate (BRL 49653) 是一种噻唑烷二酮类抗高血糖药，是PPARγ的高亲和、选择性的激动剂，IC50为42 nM。Rosiglitazone maleate 也能调节 TRP channels并诱导自噬。Rosiglitazone 可预防铁死亡。	Cell Death Dis, 2020, 11(9):752 Virol Sin, 2019, 34(6):648-661 Drugs R D, 2017, 10.1007/s40268-016-0166-4	Total and phosphorylated Akt were detected by western blot in protein lysates of liver, inguinal WAT and gastrocnemius muscle from mice that were treated with an insulin bolus after an overnight fast.
S2556	Rosiglitazone Rosiglitazone (BRL 49653) 是有效的降糖药，也是有效的噻唑烷二酮类胰岛素增敏剂，在大鼠，3T3-L1和人体脂肪细胞中IC50分别为12，4和9 nM。Rosiglitazone是PPAR-gamma的配体，对PPAR-alpha没有结合力。Rosiglitazone 可调控 TRP channels 并诱导自噬。Rosiglitazone可阻止铁死亡。	Nat Commun, 2020, 11(1):71 Cell Death Dis, 2020, 11(9):752 Cancer Cell Int, 2020, 19;20:58
S2590	Pioglitazone Pioglitazone 是一种选择性过氧化物酶体增殖物激活受体γ (PPARγ) 激动剂，用于治疗糖尿病。是全长hPPARα的弱激活剂，对全长hPPARδ没有作用。	Cancer Lett, 2020, 476:34-47 Front Immunol, 2020, 11:1224 FEBS J, 2020, 287(3):529-545	PPARγ activation, but not PPARα activation, increases β-klotho expression and FGF21 signaling. Protein (A) levels of β-klotho in hepatocytes after stimulation with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h
S8020	GW0742 GW0742是一种有效的，选择性PPARβ/δ激动剂，IC50为1 nM，比作用于hPPARα和hPPARγ选择性高1000倍。	Cells, 2019, 8(12) Int J Med Sci, 2019, 16(12):1593-1603 Sci Rep, 2017, 7:45234	(b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787
S2046	Pioglitazone HCl Pioglitazone HCl (AD-4833, U-72107E) 是一种 cytochrome P450 (CYP)2C8 和 CYP3A4 酶的抑制剂。Pioglitazone HCl 抑制CYP2C8、CYP3A4和CYP2C9的Ki值分别为1.7 μM、11.8 μM和32.1 μM。Pioglitazone HCl 也是一种选择性的 peroxisome proliferator-activated receptor-gamma (PPARγ) 激动剂，对人PPARγ和小鼠PPARγ的EC50值分别为0.93 μM和0.99 μM。Pioglitazone HCl 可抑制线粒体内铁的摄取、脂质过氧化和随后的铁死亡。	Biol Pharm Bull, 2019, 42(8):1303-1309 Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Drug Metab Dispos, 2013, 42(3):318-22	Primary hepatocytes were treated with or without 20μM Wy14643/Pioglitazone/Rosiglitazone for 24h followed by stimulation with or without 1μg/ml recombinant human FGF21 for 15min. FGF21 signaling was analyzed by phosphorylation of ERK1/2 and FRS2 examination.
S2665	Ciprofibrate Ciprofibrate (Win-35833)是一种过氧化物酶体增殖物激活受体激动剂。	Respir Physiol Neurobiol, 2020, 271:103290
S4159	Bezafibrate Bezafibrate (BM 15075) 是第一个临床测试的双重pan-peroxisome proliferator-activated receptors (PPAR)（过氧化物酶体增殖物激活受体）联合激动剂。
S4207	Clofibric Acid Clofibric acid 是PPARα激动剂，是一种降血脂剂。
S1794	Fenofibrate Fenofibrate 是一种Fibrate类化合物，是纤维酸衍生物。Fenofibrate 是 PPARα 的选择性激动剂，EC50为30μM。Fenofibrate 可结合并抑制 cytochrome P450 epoxygenase (CYP)2C ，对于CYP2C19、CYP2B6和CYP2C9的IC50分别为0.2 μM、0.7 μM和9.7 μM。Fenofibrate 可诱导自噬。	J Cell Mol Med, 2020, 24(6):3384-3398 Cancer Discov, 2020, CD-20-0160 Int J Biol Macromol, 2019, 134:759-769	E. The mTOR-lipin1-SREBP1 pathway in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate (25 mg/kg) or vehicle (H2O) for 8 days. F. mRNA expression of key genes in lipid metabolism in the liver of the Rab8af/f and Rab8a-mKO female mice gavaged with fenofibrate or vehicle for 8 days. n = 4-6. Statistical analyses were carried out using two-way ANOVA. * indicates p <0.05. n.s., not significant.
S2075	Rosiglitazone HCl Rosiglitazone HCl是一种降血糖药物，通过在脂肪细胞中与PPAR受体结合而刺激胰岛素分泌。	Cell Death Dis, 2020, 11(9):752 Reprod Toxicol, 2016, 61:162-8 Toxicol Appl Pharmacol, 2015, 285(1):51-60
S9199	Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S8770	Lanifibranor (IVA-337) Lanifibranor (IVA-337)是一种泛PPAR激动剂，对hPPARα、hPPARδ 和 hPPARγ的EC50值分别为1537 nM、866 nM和206 nM。
S3846	Eupatilin Eupatilin (NSC 122413), a major flavonoid from Artemisia plants, possesses various beneficial biological effects including anti-inflammation, anti-tumor, anti-cancer, anti-allergy, and anti-oxidation activity.	Clin Exp Reprod Med, 2020, 47(2):108-113
S3786	Glabridin Glabridin, one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
S8432	Troglitazone (CS-045) Troglitazone (Rezulin, Romglizone, Prelay, CS045, Romozin) 是PPAR的有效激动剂，PPAR是配体激活的转录因，可参与调解细胞分化和生长。Troglitazone 诱导膀胱癌细胞自噬、凋亡和坏死。Troglitazone 可在Pfa1细胞中防止RSL3诱导的铁死亡和脂质过氧化。	Nat Commun, 2019, 11;10(1):4621
S3878	Bavachinin Bavachinin (7-O-Methylbavachin) ia a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50 = 0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
S5812	Choline Fenofibrate Choline fenofibrate是一种非诺贝特酸的胆碱盐，非诺贝特酸是一种合成的苯氧异丁酸衍生物，具有抗高血脂活性，是PPARα激动剂。
S3720	Elafibranor Elafibranor (GFT505) 是PPAR-alpha和PPAR-δ的激动剂，改善胰岛素敏感度、有益于葡萄糖稳态、脂质代谢并减少炎症。
S9480	Raspberry Ketone Raspberry ketone是一种天然存在的酚类化合物，是红莓中的主要芳香化合物。
S5615	Cardarine (GW501516) Cardarine (GW501516, Cardarine, GW1516) is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.

目录号	产品描述	文献引用
S6906^New	Capric acid Capric acid (DA, Decanoic acid, Decylic acid) 是在椰子油和棕榈油中天然存在的中链甘油三酯的成分，可通过直接抑制 AMPA receptor 来控制癫痫发作。癸酸还是 PPARs 的调节配体。由于其特殊的熔化范围，产品可能是固体、液体或半固体状态。
S7955	EPI-001 EPI-001是androgen receptor N-端结构域的拮抗剂，也是一种选择性PPAR-gamma调节剂。	Prostate, 2019, 79(2):206-214
S3834	Astaxanthin Astaxanthin, a xanthophyll carotenoid, is a nutrient with unique cell membrane actions and diverse clinical benefits with excellent safety and tolerability.	Aging (Albany NY), 2019, 11(22):10513-10531 Nature, 2018, 560(7718):372-376
S3868	Harmine Harmine is an alkaloid of the β-carboline family that regulates PPARγ expression through inhibition of the Wnt signaling pathway. It also selectively binds to MAO-A and reversibly inhibits monoamine oxidase A (MAO-A) but not the variant MAO-B.	Cell Death Dis, 2019, 10(12):899

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