PPAR

信号通路图

研究领域

抑制剂选择性比较
溶解性比较

目录号	产品目录	溶解度(25°C)
目录号	产品目录	水	DMSO	酒精
S2871	T0070907	<1 mg/mL	26 mg/mL	<1 mg/mL
S7767	AZ6102	<1 mg/mL	85 mg/mL	<1 mg/mL
S7484	FH535	<1 mg/mL	72 mg/mL	<1 mg/mL
S4527	Fenofibric acid	63 mg/mL	63 mg/mL	63 mg/mL
S9189	Oroxin A	-1 mg/mL	86 mg/mL	-1 mg/mL
S9177	Gypenoside XLIX	-1 mg/mL	100 mg/mL	-1 mg/mL
S8029	WY-14643 (Pirinixic Acid)	<1 mg/mL	64 mg/mL	52 mg/mL
S1729	Gemfibrozil	<1 mg/mL	50 mg/mL	50 mg/mL
S4708	Palmitoylethanolamide	<1 mg/mL	59 mg/mL	59 mg/mL
S2915	GW9662	<1 mg/mL	55 mg/mL	<1 mg/mL
S5817	GSK0660	<1 mg/mL	84 mg/mL	<1 mg/mL
S8025	GSK3787	<1 mg/mL	79 mg/mL	<1 mg/mL
S2505	Rosiglitazone maleate	<1 mg/mL	94 mg/mL	<1 mg/mL
S2556	Rosiglitazone	<1 mg/mL	71 mg/mL	<1 mg/mL
S2590	Pioglitazone	<1 mg/mL	10 mg/mL	<1 mg/mL
S5812	Choline Fenofibrate	9 mg/mL	5 mg/mL	7 mg/mL
S8770	Lanifibranor(IVA-337)	<1 mg/mL	87 mg/mL	<1 mg/mL
S9199	Pseudoginsenoside F11	-1 mg/mL	100 mg/mL	-1 mg/mL
S5615	Cardarine (GW501516)	-1 mg/mL	90 mg/mL	-1 mg/mL
S3878	Bavachinin	-1 mg/mL	67 mg/mL	-1 mg/mL
S8020	GW0742	<1 mg/mL	94 mg/mL	44 mg/mL
S2665	Ciprofibrate	<1 mg/mL	58 mg/mL	58 mg/mL
S4159	Bezafibrate	<1 mg/mL	72 mg/mL	18 mg/mL
S4207	Clofibric Acid	<1 mg/mL	43 mg/mL	43 mg/mL
S1794	Fenofibrate	<1 mg/mL	72 mg/mL	46 mg/mL
S2075	Rosiglitazone HCl	<1 mg/mL	79 mg/mL	79 mg/mL
S3786	Glabridin	-1 mg/mL	64 mg/mL	-1 mg/mL
S8432	Troglitazone (CS-045)	<1 mg/mL	88 mg/mL	15 mg/mL
S3720	Elafibranor	<1 mg/mL	76 mg/mL	76 mg/mL
S3868	Harmine	-1 mg/mL	42 mg/mL	-1 mg/mL

特异性亚型抑制剂

PPAR抑制剂（31）
新PPAR产品

产品目录	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。	Aging Cell, 2018, 10.1111/acel.12774 Cell Death Dis, 2017, 8(1):e2553 J Neuroinflammation, 2014, 12:51	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）。
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。	Oncogenesis, 2017, 6(3):e300 Int J Clin Exp Pathol, 2016, 9(3):2857-2868 Cancer Med, 2018, 7(2):285-296	BrdU assay was used to detect the proliferation level of cells in four groups: the control group, FH535 (15 μM) group, NAM (50 mM) + FH535 (15 μM) group, REV (100 μM) + FH535 (15 μM) group. A. At the next day, the cells were fixed and immunostained for BrdU (red) and with DAPI (blue) then merged the two pictures of the same field. The scale bar is 100 μm. B. The total numbers of cells (DAPI-staining cells) per field in the four groups. C. BrdU-positive rate of C2C12 cells was analyzed. Each value represents the mean ± standard error of the mean of triplicate determinations from three independent cell preparations. P<0.05, P<0.01, **P<0.001 vs the value of the control; n=3; error bars ± standard error of means. Statistical analysis was conducted using one-way ANOVA. Original magnification is ×200.
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。
S9189^New	Oroxin A Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
S9177^New	Gypenoside XLIX Gypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator.
S8029	WY-14643 (Pirinixic Acid) WY-14643 (Pirinixic Acid)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。	Diabetes, 2017, 66(8):2112-2123	(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 是一种降低血脂水平的化合物。
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.
S4708	Palmitoylethanolamide Palmitoylethanolamide(PEA)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。
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。	Theranostics, 2018, 8(15):4262-4278 Toxicol Appl Pharmacol, 2016, 316:17-26 Fish Shellfish Immunol, 2015, 43(2):310-324	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.
S5817^New	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。
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。	Neuropharmacology, 2017, 113(Pt A):396-406 Int Immunopharmacol, 2016, 40:73-78	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.
S2505	Rosiglitazone maleate Rosiglitazone maleate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。	Mol Metab, 2013, 2(3):215-26 Toxicol Appl Pharmacol, 2015, 285(1):51-60 Reprod Toxicol, 2016, 61:162-8	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。	J Leukoc Biol, 2014, 95(4):587-98 Toxicol Appl Pharmacol, 2015, 285(1):51-60 Clin Exp Immunol, 2017, 189(2):211-225
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。	Mol Nutr Food Res, 2017, 10.1002/mnfr.201601075 Am J Physiol Endocrinol Metab, 2016, 311(4):E763-E771 Drug Metab Dispos, 2014, 42(3):318-22	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
S5812^New	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。
S8770^New	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。
S9199^New	Pseudoginsenoside F11 Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
S5615^New	Cardarine (GW501516) GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
S3878^New	Bavachinin Bavachinina 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).
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。	Neuropharmacology, 2016, 10.1016/j.neuropharm.2016.10.022 Sci Rep, 2017, 7:45234 Lab Invest, 2016, 96(2):218-29	(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
S2665	Ciprofibrate Ciprofibrate是一种过氧化物酶体增殖物激活受体激动剂。
S4159	Bezafibrate Bezafibrate 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。	Diabetes, 2017, 66(9):2387-2399 Food Funct, 2018, 9(12):6608-6617	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。	J Leukoc Biol, 2014, 95(4):587-98 Toxicol Appl Pharmacol, 2015, 285(1):51-60 Reprod Toxicol, 2016, 61:162-8
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。
S3720	Elafibranor Elafibranor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。
S3868^New	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.

研究领域

产品类型

PPAR

信号通路图

研究领域

特异性亚型抑制剂