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)
DMSO 酒精
S2505 Rosiglitazone maleate <1 mg/mL 94 mg/mL <1 mg/mL
S2556 Rosiglitazone <1 mg/mL 71 mg/mL <1 mg/mL
S2915 GW9662 <1 mg/mL 55 mg/mL <1 mg/mL
S2871 T0070907 <1 mg/mL 26 mg/mL <1 mg/mL
S2590 Pioglitazone <1 mg/mL 10 mg/mL <1 mg/mL
S3868 Harmine -1 mg/mL 42 mg/mL -1 mg/mL
S3878 Bavachinin -1 mg/mL 67 mg/mL -1 mg/mL
S3786 Glabridin -1 mg/mL 64 mg/mL -1 mg/mL
S3720 Elafibranor <1 mg/mL 76 mg/mL 76 mg/mL
S8029 WY-14643 (Pirinixic Acid) <1 mg/mL 64 mg/mL 52 mg/mL
S8025 GSK3787 <1 mg/mL 79 mg/mL <1 mg/mL
S8020 GW0742 <1 mg/mL 94 mg/mL 44 mg/mL
S1729 Gemfibrozil <1 mg/mL 50 mg/mL 50 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
S7767 AZ6102 <1 mg/mL 85 mg/mL <1 mg/mL
S8432 Troglitazone (CS-045) <1 mg/mL 88 mg/mL 15 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
S4708 Palmitoylethanolamide <1 mg/mL 59 mg/mL 59 mg/mL

特异性亚型抑制剂

产品目录 产品描述 文献引用 实验数据
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。

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。

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。

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。

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。

S3868New

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.

S3878New

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).

S3786New

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.

S5121New

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.

S3720New

Elafibranor

Elafibranor是PPAR-alphaPPAR-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。

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。

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。

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。

S1729

Gemfibrozil

Gemfibrozil 是一种降低血脂水平的化合物。

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。

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。

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)。

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。

S7484

FH535

FH535是一种Wnt/β-catenin信号传导抑制剂,同时也是PPARγPPARδ的双重拮抗剂。

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。

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。